ES2348576T3 - DPP INHIBITOR FORMULATIONS IV. - Google Patents
DPP INHIBITOR FORMULATIONS IV. Download PDFInfo
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- ES2348576T3 ES2348576T3 ES07728658T ES07728658T ES2348576T3 ES 2348576 T3 ES2348576 T3 ES 2348576T3 ES 07728658 T ES07728658 T ES 07728658T ES 07728658 T ES07728658 T ES 07728658T ES 2348576 T3 ES2348576 T3 ES 2348576T3
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Abstract
Una composición farmacéutica que comprende como ingrediente activo un compuesto inhibidor de DPP IV con un grupo amino seleccionado de - 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(R)-amino-piperidin-1-il)xantina, - 1-[([1,5]naftiridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, - 1-[(Quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, - 2-((R)-3-Amino-piperidin-1-il)-3-(but-2-inil)-5-(4-metil-quinazolin-2-ilmetil)-3,5dihidro-imidazo[4,5-d]piridazin-4-ona, - 1-[(4-Metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(2-amino-2-metil-propil)metilamino]-xantina, - 1-[(3-Ciano-quinolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, - 1-(2-Ciano-bencil)-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)-xantina, - 1-[(4-Metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(S)-(2-aminopropil)metilamino]-xantina, - 1-[(3-Ciano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, - 1-[(4-Metil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, - 1-[(4,6-Dimetil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1il)-xantina, y - 1-[(Quinoxalin-6-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, o una sal de estos, un primer diluyente que es manitol, un segundo diluyente que es almidón pregelatinizado, un aglutinante que es copovidona, un disgregante que es almidón de maíz, y un lubricante que es estearato de magnesio.A pharmaceutical composition comprising as active ingredient a DPP IV inhibitor compound with an amino group selected from - 1 - [(4-methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1 -il) -8- (3- (R) -amino-piperidin-1-yl) xanthine, - 1 - [([1,5] naphthyridin-2-yl) methyl] -3-methyl-7- (2 -butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine, - 1 - [(Quinazolin-2-yl) methyl] -3-methyl-7- (2- butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine, - 2 - ((R) -3-Amino-piperidin-1-yl) -3- (but- 2-inyl) -5- (4-methyl-quinazolin-2-ylmethyl) -3,5dihydro-imidazo [4,5-d] pyridazin-4-one, - 1 - [(4-Methyl-quinazolin-2- il) methyl] -3-methyl-7- (2-butin-1-yl) -8 - [(2-amino-2-methyl-propyl) methylamino] -xanthine, - 1 - [(3-Cyano-quinolin -2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine, - 1- (2-Cyano -benzyl) -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) -xanthine, - 1 - [(4-Methyl-quinazolin -2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - [(S) - (2-aminopropyl) methylamino] -xanthine, - 1 - [(3-Cyano- pyridin-2-yl) methyl] -3-methyl-7- (2-b utin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine, - 1 - [(4-Methyl-pyrimidin-2-yl) methyl] -3-methyl-7- (2-Butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine, - 1 - [(4,6-Dimethyl-pyrimidin-2-yl) methyl] -3 -methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1yl) -xanthine, and - 1 - [(Quinoxalin-6-yl) methyl] -3- methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine, or a salt thereof, a first diluent that is mannitol, a second diluent that it is pregelatinized starch, a binder that is copovidone, a disintegrant that is corn starch, and a lubricant that is magnesium stearate.
Description
La presente invención se refiere a composiciones farmacéuticas de inhibidores de DPP IV seleccionados, a su preparación y a su uso para tratar condiciones médicas seleccionadas. The present invention relates to pharmaceutical compositions of selected DPP IV inhibitors, their preparation and their use to treat selected medical conditions.
La enzima DPP-IV (dipeptidil peptidasa IV), conocida también como CD26, es una serina proteasa que se sabe que dirige la escisión de un dipéptido del extremo N-terminal de una serie de proteínas que tienen en su extremo N-terminal un resto de prolina o de alanina. Debido a esta propiedad, los inhibidores de DPP-IV interfieren con el nivel plasmático de los péptidos bioactivos que incluyen el péptido GLP-1, y se considera que son fármacos prometedores para el tratamiento de la diabetes mellitus. The DPP-IV enzyme (dipeptidyl peptidase IV), also known as CD26, is a serine protease that is known to direct the cleavage of a dipeptide from the N-terminal end of a series of proteins that have a residue at their N-terminal end. of proline or alanine. Due to this property, DPP-IV inhibitors interfere with the plasma level of bioactive peptides that include the GLP-1 peptide, and are considered to be promising drugs for the treatment of diabetes mellitus.
En un intento de preparar composiciones farmacéuticas de inhibidores de DPPIV seleccionados, se ha observado que los inhibidores de DPP-IV con un grupo amino primario o secundario muestran incompatibilidades, problemas de degradación o problemas de extracción con numerosos excipientes habituales tales como celulosa microcristalina, glicolato sódico de almidón, croscarmelosa sódica, ácido tartárico, ácido cítrico, glucosa, fructosa, sacarosa, lactosa o maltodextrinas. Aunque los propios compuestos son muy estables, reaccionan con muchos excipientes utilizados en las formas de dosificación sólidas y con las impurezas de los excipientes, especialmente en el estrecho contacto proporcionado en los comprimidos y en las proporciones elevadas excipiente/fármaco. El grupo amino parece reaccionar con los azúcares reductores y con otros grupos carbonilo reactivos y con los grupos funcionales de ácido carboxílico formados, por ejemplo, en la superficie de la celulosa microcristalina por oxidación. Estas dificultades imprevistas se observan principalmente en los intervalos de dosis bajas que se requieren debido a la sorprendente potencia de los inhibidores seleccionados. Por lo tanto, se requieren composiciones farmacéuticas para resolver estos problemas técnicos asociados con la potencia inesperada de los compuestos inhibidores de DPP-IV seleccionados. In an attempt to prepare pharmaceutical compositions of selected DPPIV inhibitors, it has been observed that DPP-IV inhibitors with a primary or secondary amino group show incompatibilities, degradation problems or extraction problems with numerous common excipients such as microcrystalline cellulose, glycolate starch sodium, croscarmellose sodium, tartaric acid, citric acid, glucose, fructose, sucrose, lactose or maltodextrins. Although the compounds themselves are very stable, they react with many excipients used in solid dosage forms and with the impurities of the excipients, especially in the close contact provided in the tablets and in the high excipient / drug ratios. The amino group appears to react with the reducing sugars and with other reactive carbonyl groups and with the carboxylic acid functional groups formed, for example, on the surface of the microcrystalline cellulose by oxidation. These unforeseen difficulties are mainly observed in the low dose intervals that are required due to the surprising potency of the selected inhibitors. Therefore, pharmaceutical compositions are required to solve these technical problems associated with the unexpected potency of the selected DPP-IV inhibitor compounds.
Una composición farmacéutica según la presente invención se pretende para el tratamiento para conseguir el control glucémico en un paciente con diabetes mellitus tipo 1 o tipo 2 y comprende un inhibidor de DPP-IV con un grupo amino, especialmente un grupo amino libre o primario, como ingrediente activo, un primer y segundo diluyente, un aglutinante, un disgregante y un lubricante. Una opción adicional es un disgregante adicional y un deslizante adicional. Adicionalmente, las composiciones se pueden utilizar para tratar la artritis reumatoide, la obesidad y la osteoporosis, así como para fortalecer el transplante de aloinjerto. A pharmaceutical composition according to the present invention is intended for treatment to achieve glycemic control in a patient with type 1 or type 2 diabetes mellitus and comprises a DPP-IV inhibitor with an amino group, especially a free or primary amino group, such as active ingredient, a first and second diluent, a binder, a disintegrant and a lubricant. An additional option is an additional disintegrant and an additional slider. Additionally, the compositions can be used to treat rheumatoid arthritis, obesity and osteoporosis, as well as to strengthen allograft transplantation.
Los diluyentes adecuados para una composición farmacéutica según la invención son polvo de celulosa, fosfato de calcio dibásico anhidro, fosfato de calcio dibásico dihidrato, eritriol, hidroxipropilcelulosa poco sustituida, manitol, almidón pregelatinizado o xilitol. Entre estos diluyentes se prefieren manitol y almidón pregelatinizado. Suitable diluents for a pharmaceutical composition according to the invention are cellulose powder, anhydrous dibasic calcium phosphate, dibasic calcium phosphate dihydrate, erythriol, low substituted hydroxypropylcellulose, mannitol, pregelatinized starch or xylitol. Among these diluents, mannitol and pregelatinized starch are preferred.
Los diluyentes preferidos como segundo diluyente son los diluyentes mencionados anteriormente almidón pregelatinizado e hidroxipropilcelulosa poco sustituida (L-HPC) que muestran propiedades aglutinantes adicionales. Preferred diluents as the second diluent are the above-mentioned diluents pregelatinized starch and low substituted hydroxypropylcellulose (L-HPC) which show additional binding properties.
Los lubricantes adecuados para una composición farmacéutica según la invención son talco, polietilenglicol, behenato de calcio, estearato de calcio, aceite de ricino hidrogenado o estearato de magnesio. El lubricante preferido es estearato de magnesio. Suitable lubricants for a pharmaceutical composition according to the invention are talc, polyethylene glycol, calcium behenate, calcium stearate, hydrogenated castor oil or magnesium stearate. The preferred lubricant is magnesium stearate.
Los aglutinantes adecuados para una composición farmacéutica según la invención son copovidona (copolimerizados de vinilpirrolidona con otros derivados de vinilo), hidroxipropil metilcelulosa (HPMC), hidroxipropilcelulosa (HPC), polivinilpirrolidona (povidona), almidón pregelatinizado, hidroxipropilcelulosa poco sustituida (L-HPC), prefiriéndose copovidona y almidón pregelatinizado. Suitable binders for a pharmaceutical composition according to the invention are copovidone (copolymerized from vinyl pyrrolidone with other vinyl derivatives), hydroxypropyl methylcellulose (HPMC), hydroxypropylcellulose (HPC), polyvinylpyrrolidone (povidone), pregelatinized starch, hydroxypropylcellulose (hydroxypropylcellulose) , with copovidone and pregelatinized starch being preferred.
Los aglutinantes mencionados anteriormente, almidón pregelatinizado y L-HPC muestran propiedades adicionales de diluyente y disgregante y se pueden usar también como el segundo diluyente o como el disgregante. The binders mentioned above, pregelatinized starch and L-HPC show additional properties of diluent and disintegrant and can also be used as the second diluent or as the disintegrant.
Los disgregantes adecuados para una composición farmacéutica según la presente invención son almidón de maíz, crospovidona, hidroxipropilcelulosa poco sustituida (L-HPC) o almidón pregelatinizado, prefiriéndose almidón de maíz. Suitable disintegrants for a pharmaceutical composition according to the present invention are corn starch, crospovidone, low substituted hydroxypropyl cellulose (L-HPC) or pregelatinized starch, with corn starch being preferred.
Como deslizante opcional puede usarse dióxido de silicio coloidal. As an optional slider, colloidal silicon dioxide can be used.
Una composición ejemplar según la presente invención comprende el diluyente manitol, almidón pregelatinizado como diluyente con propiedades aglutinantes adicionales, el aglutinante copovidona, el disgregante almidón de maíz, y estearato de magnesio como lubricante. An exemplary composition according to the present invention comprises the mannitol diluent, pregelatinized starch as a diluent with additional binding properties, the copovidone binder, the corn starch disintegrant, and magnesium stearate as a lubricant.
Las formas de dosificación preparadas con una composición farmacéutica según la presente invención contienen ingredientes activos en los intervalos de dosificación de 0,1-100 mg. Las dosificaciones preferidas son 0,5 mg, 1 mg, 2,5 mg, 5 mg y 10 mg. Dosage forms prepared with a pharmaceutical composition according to the present invention contain active ingredients in the dosage ranges of 0.1-100 mg. Preferred dosages are 0.5 mg, 1 mg, 2.5 mg, 5 mg and 10 mg.
Las composiciones farmacéuticas típicas comprenden (% en peso) Typical pharmaceutical compositions comprise (% by weight)
0,5-20 % ingrediente activo 40-88 % diluyente 1, 3-40 % diluyente 2, 1-5 % aglutinante, 5-15 % disgregante, y 0,1-4 % lubricante. 0.5-20% active ingredient 40-88% diluent 1, 3-40% diluent 2, 1-5% binder, 5-15% disintegrating, and 0.1-4% lubricant.
Las composiciones farmacéuticas preferidas comprenden (% en peso) 0,5-7 % ingrediente activo 50-75 % diluyente 1, 5-15 % diluyente 2, 2-4 % aglutinante, 8-12 % disgregante, y 0,5-2 % lubricante Preferred pharmaceutical compositions comprise (% by weight) 0.5-7% active ingredient 50-75% diluent 1, 5-15% diluent 2, 2-4% binder, 8-12% disintegrating, and 0.5-2% lubricant
5 Las composiciones farmacéuticas según la invención se pretenden para uso oral y pueden usarse en la forma de dosificación de una cápsula, un comprimido o un comprimido recubierto de una película. Típicamente el recubrimiento pelicular representa el 2-4%, preferiblemente el 3% de la composición y comprende un agente formador de película, un plastificante, un deslizante y opcionalmente uno o más The pharmaceutical compositions according to the invention are intended for oral use and can be used in the dosage form of a capsule, a tablet or a film-coated tablet. Typically the film coating represents 2-4%, preferably 3% of the composition and comprises a film-forming agent, a plasticizer, a slider and optionally one or more
10 pigmentos. Una composición de recubrimiento ejemplar puede comprender hidroxipropilmetilcelulosa (HPMC), polietilen glicol (PEG), talco, dióxido de titanio y opcionalmente óxido de hierro. 10 pigments An exemplary coating composition may comprise hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG), talc, titanium dioxide and optionally iron oxide.
Los ingredientes activos preferidos en el contexto de la presente invención son inhibidores de DPP-IV con un grupo amino primario y sales de estos tales como 15 cualquier inhibidor de DPP-IV y sal de éste definidos por la fórmula (I) Preferred active ingredients in the context of the present invention are DPP-IV inhibitors with a primary amino group and salts thereof such as any DPP-IV inhibitor and salt thereof defined by formula (I)
o fórmula (II) or formula (II)
en las que R1 es ([1,5]naftiridin-2-il)metilo, (quinazolin-2-il)metilo], (quinoxalin-6il)metilo, (4-Metil-quinazolin-2-il)metilo, 2-Ciano-bencilo, (3-Ciano-quinolin-2-il)metilo, (3-Ciano-piridin-2-il)metilo, (4-Metil-pirimidin-2-il)metilo o (4,6-Dimetil-pirimidin-2wherein R 1 is ([1,5] naphthyridin-2-yl) methyl, (quinazolin-2-yl) methyl], (quinoxalin-6-yl) methyl, (4-Methyl-quinazolin-2-yl) methyl, 2 -Cyan-benzyl, (3-Cyano-quinolin-2-yl) methyl, (3-Cyano-pyridin-2-yl) methyl, (4-Methyl-pyrimidin-2-yl) methyl or (4,6-Dimethyl -pyrimidin-2
5 il)metilo, y R2 es 3-(R)-amino-piperidin-1-ilo, (2-amino-2-metil-propil)-metilamino o (2(S)-amino-propil)-metilamino. Los compuestos inhibidores de DPP IV preferidos son los compuestos siguientes y las sales de estos: 5-yl) methyl, and R2 is 3- (R) -amino-piperidin-1-yl, (2-amino-2-methyl-propyl) -methylamino or (2 (S) -amino-propyl) -methylamino. Preferred DPP IV inhibitor compounds are the following compounds and salts thereof:
• 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(R)-amino-piperidin-1-il)10 xantina (compárese con WO 2004/018468, ejemplo 2(142)): • 1 - [(4-methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8- (3- (R) -amino-piperidin-1-yl ) 10 xanthine (compare WO 2004/018468, example 2 (142)):
• 1-[([1,5]naftiridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina (compárese con WO 2004/018468, ejemplo 2(252)): • 1 - [([1,5] naphthyridin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1- il) xanthine (compare WO 2004/018468, example 2 (252)):
15 • 1-[(Quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina (compárese con WO 2004/018468, ejemplo 2(80)): 15 • 1 - [(Quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine ( compare WO 2004/018468, example 2 (80)):
- • •
- 2-((R)-3-Amino-piperidin-1-il)-3-(but-2-inil)-5-(4-metil-quinazolin-2-ilmetil)-3,5dihidro-imidazo[4,5-d]piridazin-4-ona (compárese con WO 2004/050658, ejemplo 136): 2 - ((R) -3-Amino-piperidin-1-yl) -3- (but-2-inyl) -5- (4-methyl-quinazolin-2-ylmethyl) -3,5-dihydro-imidazo [4, 5-d] pyridazin-4-one (compare WO 2004/050658, example 136):
- • •
- 1-[(4-Metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(2-amino-2-metil-propil)metilamino]-xantina (compárese con WO 2006/029769, ejemplo 2(1)): 1 - [(4-Methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - [(2-amino-2-methyl-propyl) methylamino] - xanthine (compare WO 2006/029769, example 2 (1)):
- • •
- 1-[(3-Ciano-quinolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina (compárese con WO 2005/085246, ejemplo 1(30)): 1 - [(3-Cyano-quinolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine (compare WO 2005/085246, example 1 (30)):
- • •
- 1-(2-Ciano-bencil)-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)-xantina (compárese con WO 2005/085246, ejemplo 1(39)): 1- (2-Cyano-benzyl) -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) -xanthine (compare WO 2005 / 085246, example 1 (39)):
- • •
- 1-[(4-Metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(S)-(2-aminopropil)metilamino]-xantina (compárese con WO 2006/029769, ejemplo 2(4)): 1 - [(4-Methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - [(S) - (2-aminopropyl) methylamino] -xanthine ( compare WO 2006/029769, example 2 (4)):
- • •
- 1-[(3-Ciano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina (compárese con WO 2005/085246, ejemplo 1(52)): 1 - [(3-Cyano-pyridin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine (compare WO 2005/085246, example 1 (52)):
- • •
- 1-[(4-Metil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina (compárese con WO 2005/085246, ejemplo 1(81)): 1 - [(4-Methyl-pyrimidin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine (compare WO 2005/085246, example 1 (81)):
- • •
- 1-[(4,6-Dimetil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1il)-xantina (compárese con WO 2005/085246, ejemplo 1(82)): 1 - [(4,6-Dimethyl-pyrimidin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1il) -xanthine (compare WO 2005/085246, example 1 (82)):
- • •
- 1-[(Quinoxalin-6-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina (compárese con WO 2005/085246, ejemplo 1(83)). 1 - [(Quinoxalin-6-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine (compare WO 2005/085246, example 1 (83)).
5 5
Para preparar las composiciones según la invención puede prepararse un granulado por un proceso de granulación húmeda. Los métodos alternativos para la granulación del ingrediente activo y los excipientes con un líquido de granulación son granulación en lecho fluido o granulación en un recipiente. To prepare the compositions according to the invention a granulate can be prepared by a wet granulation process. Alternative methods for granulation of the active ingredient and excipients with a granulation liquid are fluid bed granulation or granulation in a container.
10 En el proceso de granulación húmeda el líquido de granulación es un disolvente tal como agua, etanol, metanol, isopropanol, acetona, preferiblemente agua purificada, y contiene un aglutinante tal como copovidona. El disolvente es un componente volátil que no queda en el producto final. El ingrediente activo y los demás excipientes con excepción del lubricante se mezclan previamente y se granulan con el In the wet granulation process the granulation liquid is a solvent such as water, ethanol, methanol, isopropanol, acetone, preferably purified water, and contains a binder such as copovidone. The solvent is a volatile component that is not left in the final product. The active ingredient and the other excipients with the exception of the lubricant are pre-mixed and granulated with the
15 líquido de granulación acuoso usando un granulador de cizallamiento alto. La etapa de granulación húmeda es seguida de una etapa opcional de tamizado húmedo, secado y tamizado en seco de los gránulos. Por ejemplo se puede utilizar para el secado un secador de lecho fluido. Los gránulos secos se tamizan a través de un tamiz apropiado. Después de la 15 aqueous granulation liquid using a high shear granulator. The wet granulation stage is followed by an optional wet sieving, drying and dry sieving stage of the granules. For example, a fluid bed dryer can be used for drying. The dried granules are screened through an appropriate sieve. After the
20 adición de los demás excipientes con excepción del lubricante la mezcla se mezcla en un mezclador convencional adecuado tal como un mezclador de caída libre seguido de la adición del lubricante tal como estearato de magnesio y mezclado final en el mezclador. Así, un proceso de granulación húmeda ejemplar para la preparación de una In addition to the other excipients other than the lubricant, the mixture is mixed in a suitable conventional mixer such as a free fall mixer followed by the addition of the lubricant such as magnesium stearate and final mixing in the mixer. Thus, an exemplary wet granulation process for the preparation of a
25 composición farmacéutica según la presente invención comprende The pharmaceutical composition according to the present invention comprises
- a. to.
- disolver un aglutinante tal como copovidona en un disolvente tal como agua purificada a temperatura ambiente para producir un líquido de granulación; dissolving a binder such as copovidone in a solvent such as purified water at room temperature to produce a granulation liquid;
- b. b.
- mezclar un inhibidor de DPP-IV, un diluyente y un disgregante en un mezclador adecuado, para producir una pre-mezcla; mixing a DPP-IV inhibitor, a diluent and a disintegrant in a suitable mixer, to produce a pre-mix;
- c. C.
- humedecer la pre-mezcla con el líquido de granulación y seguidamente granular la pre-mezcla humedecida, por ejemplo en un mezclador de cizallamiento alto; moisten the pre-mix with the granulation liquid and then granulate the moistened pre-mix, for example in a high shear mixer;
- d. d.
- opcionalmente tamizar la pre-mezcla granulada a través de un tamiz con un tamaño de malla de al menos 1,0 mm y preferiblemente de 3 mm; optionally sieving the granulated pre-mix through a screen with a mesh size of at least 1.0 mm and preferably 3 mm;
- e. and.
- secar el granulado a aproximadamente 40-750C y preferiblemente 55-650C de temperatura del aire de entrada por ejemplo en un secador de lecho fluido hasta que se obtenga la pérdida deseada en el valor de secado en el intervalo de 1-5 %; drying the granulate at approximately 40-750C and preferably 55-650C inlet air temperature for example in a fluid bed dryer until the desired loss in the drying value in the range of 1-5% is obtained;
- f. F.
- deshacer los terrones del granulado seco, por ejemplo tamizando a través de un tamiz con un tamaño de malla de 0,6 mm-1,6 mm, preferiblemente 1,0 mm; y undo the lumps of the dried granulate, for example by sieving through a sieve with a mesh size of 0.6 mm-1.6 mm, preferably 1.0 mm; Y
- g. g.
- añadir preferiblemente lubricante tamizado al granulado para el mezclado final por ejemplo en un mezclador cúbico. preferably add sieved lubricant to the granulate for final mixing, for example in a cubic mixer.
En un proceso alternativo parte de los excipientes tal como parte de un disgregante (p.ej. almidón de maíz) o un diluyente (p.ej. almidón pregelatinizado) o un disgregante adicional (crospovidona) puede añadirse de manera extragranular antes del mezclado final de la etapa g. In an alternative process part of the excipients such as part of a disintegrant (eg corn starch) or a diluent (eg pregelatinized starch) or an additional disintegrant (crospovidone) can be added extragranularly before final mixing of stage g.
En otra versión alternativa del proceso, el granulado producido en las etapas a a e se produce en un proceso de granulación de cizallamiento alto en un solo recipiente y posteriormente se seca en un granulador con un solo recipiente. In another alternative version of the process, the granulate produced in steps a to e is produced in a high shear granulation process in a single container and subsequently dried in a granulator with a single container.
Para la preparación de las cápsulas, la mezcla final se usa para rellenar cápsulas. For the preparation of the capsules, the final mixture is used to fill capsules.
Para la preparación de comprimidos o núcleos de comprimidos, la mezcla final se comprime además en comprimidos con el peso diana del núcleo del comprimido con un tamaño y resistencia a la compresión apropiados, usando una prensa de comprimidos apropiada. For the preparation of tablets or tablet cores, the final mixture is further compressed into tablets with the target weight of the tablet core with an appropriate size and compressive strength, using an appropriate tablet press.
Para la preparación de los comprimidos recubiertos con película, se prepara una suspensión de recubrimiento y los núcleos comprimidos de los comprimidos se recubren con la suspensión de recubrimiento hasta una ganancia de peso de aproximadamente 2-4 %, preferiblemente aproximadamente 3 %, utilizando un equipo estándar de recubrimiento con película. El disolvente del recubrimiento con película es un componente volátil, que no permanece en el producto final. Para reducir la cantidad requerida de lubricante en los comprimidos una opción es utilizar un sistema de lubricación externa. For the preparation of the film-coated tablets, a coating suspension is prepared and the compressed cores of the tablets are coated with the coating suspension to a weight gain of about 2-4%, preferably about 3%, using equipment Standard coating with film. The film coating solvent is a volatile component, which does not remain in the final product. To reduce the required amount of lubricant in tablets an option is to use an external lubrication system.
Ejemplos Examples
5 5
Un ingrediente activo de inhibidor de DPP IV con un grupo primario y todos los demás excipientes con excepción del estearato de magnesio se mezclan en un mezclador de cizallamiento alto. Esta pre-mezcla se tamiza a través de un tamiz de 1 An active ingredient of DPP IV inhibitor with a primary group and all other excipients other than magnesium stearate is mixed in a high shear mixer. This pre-mix is screened through a 1 sieve
10 mm. Después de la adición del estearato de magnesio, la pre-mezcla se mezcla en un mezclador de caída libre para producir la mezcla final. La mezcla final se comprime en comprimidos usando una prensa de comprimidos adecuada. Pueden obtenerse las composiciones siguientes: 10 mm After the addition of magnesium stearate, the pre-mixture is mixed in a free fall mixer to produce the final mixture. The final mixture is compressed into tablets using a suitable tablet press. The following compositions can be obtained:
- Componente Component
- mg/comprimido %/comprimido mg/comprimido %/comprimido mg / tablet %/compressed mg / tablet %/compressed
- Ingrediente activo Manitol Almidón pregelatinizado Estearato de magnesio Active ingredient Mannitol Pregelatinized starch Magnesium stearate
- 1,000 43,250 5,000 0,750 2,000 86,500 10,000 1,500 2,500 108,125 12,500 1,875 2,000 86,500 10,000 1,500 1,000 43,250 5,000 0,750 2,000 86,500 10,000 1,500 2,500 108,125 12,500 1,875 2,000 86,500 10,000 1,500
- Total Total
- 50,000 100,000 125,000 100,000 50,000 100,000 125,000 100,000
- Componente Component
- mg/comprimido %/comprimido mg/comprimido %/comprimido mg / tablet %/compressed mg / tablet %/compressed
- Ingrediente activo Manitol Almidón pregelatinizado Estearato de magnesio Active ingredient Mannitol Pregelatinized starch Magnesium stearate
- 5,000 216,250 25,000 3,750 2,000 86,500 10,000 1,500 10,000 432,500 50,000 7,500 2,000 86,500 10,000 1,500 5,000 216,250 25,000 3,750 2,000 86,500 10,000 1,500 10,000 432,500 50,000 7,500 2,000 86,500 10,000 1,500
- Total Total
- 250,000 100,000 500,000 100,000 250,000 100,000 500,000 100,000
Un ingrediente activo de inhibidor de DPP IV con un grupo primario y todos los demás excipientes con excepción del estearato de magnesio se mezclan en un mezclador de cizallamiento alto. Esta pre-mezcla se tamiza a través de un tamiz de 1 mm. Después de la adición del estearato de magnesio, la pre-mezcla se mezcla en un mezclador de caída libre para producir la mezcla final. La mezcla final se comprime en comprimidos usando una prensa de comprimidos adecuada. Pueden obtenerse las composiciones siguientes: An active ingredient of DPP IV inhibitor with a primary group and all other excipients other than magnesium stearate is mixed in a high shear mixer. This pre-mix is screened through a 1 mm sieve. After the addition of magnesium stearate, the pre-mixture is mixed in a free fall mixer to produce the final mixture. The final mixture is compressed into tablets using a suitable tablet press. The following compositions can be obtained:
- Componente Component
- mg/comprimido %/comprimido mg/comprimido %/comprimido mg / tablet %/compressed mg / tablet %/compressed
- Ingrediente activo Fosfato de calcio dibásico, anhidro Hidroxipropilcelulosa poco sustituida Estearato de magnesio Active ingredient Dibasic calcium phosphate, anhydrous Low substituted hydroxypropylcellulose Magnesium stearate
- 1,000 46,400 12,000 0,600 1,667 77,333 20,000 1,000 0,500 46,900 12,000 0,600 0,833 78,177 20,000 1,000 1,000 46,400 12,000 0.600 1,667 77,333 20,000 1,000 0.500 46.900 12,000 0.600 0.833 78.177 20,000 1,000
- Total. Total.
- 60,000 100,000 60,000 100,000 60,000 100,000 60,000 100,000
- Componente Component
- mg/comprimido %/comprimido mg/comprimido %/comprimido mg / tablet %/compressed mg / tablet %/compressed
- Ingrediente activo Fosfato de calcio dibásico, anhidro Hidroxipropilcelulosa poco sustituida Estearato de magnesio Active ingredient Dibasic calcium phosphate, anhydrous Low substituted hydroxypropylcellulose Magnesium stearate
- 10,000 464,000 120,000 6,000 1,667 77,333 20,000 1,000 10,000 344,000 90,000 6,000 2,222 76,788 20,000 1,000 10,000 464,000 120,000 6,000 1,667 77,333 20,000 1,000 10,000 344,000 90,000 6,000 2,222 76,788 20,000 1,000
- Total Total
- 600,000 100,000 450,000 100,000 600,000 100,000 450,000 100,000
Se disuelve copovidona en agua purificada a temperatura ambiente para producir un líquido de granulación. Un ingrediente activo de inhibidor de DPP IV con un grupo amino primario, manitol y parte del almidón pregelatinizado se mezclan en un Copovidone is dissolved in purified water at room temperature to produce a granulation liquid. An active ingredient of DPP IV inhibitor with a primary amino group, mannitol and part of the pregelatinized starch is mixed in a
5 mezclador adecuado, para producir una pre-mezcla. Se humedece la pre-mezcla con el líquido de granulación y se granula posteriormente. El granulado húmedo se tamiza opcionalmente a través de un tamiz con un tamaño de malla de 1,6-3.0 mm. El granulado se seca a 55ºC en un secador adecuado hasta un contenido en humedad residual correspondiente a una pérdida de 2-5 % en secado. Se tamiza el granulado 5 suitable mixer, to produce a pre-mix. The pre-mixture is moistened with the granulation liquid and subsequently granulated. The wet granulate is optionally sieved through a sieve with a mesh size of 1.6-3.0 mm. The granulate is dried at 55 ° C in a suitable dryer to a residual moisture content corresponding to a 2-5% loss in drying. The granulate is screened
10 seco a través de un tamiz con un tamaño de malla de 1,0 mm. El granulado se mezcla con parte del almidón pregelatinizado en un mezclador adecuado. Se añade estearato de magnesio a esta mezcla después de pasarla a través de un tamiz de 1,0 mm para deshacer los terrones. 10 dry through a sieve with a mesh size of 1.0 mm. The granulate is mixed with part of the pregelatinized starch in a suitable mixer. Magnesium stearate is added to this mixture after passing it through a 1.0 mm sieve to undo the lumps.
Posteriormente, se produce la mezcla final mezclando finalmente en un 15 mezclador adecuado y comprimiendo en comprimidos. Puede obtenerse la composición en comprimidos siguiente: Subsequently, the final mixture is produced by finally mixing in a suitable mixer and compressing into tablets. The following tablet composition can be obtained:
- Componente Component
- mg/comprimido %/comprimido mg / tablet %/compressed
- Ingrediente activo Active ingredient
- 10,000 1,667 10,000 1,667
- Almidón pregelatinizado Pregelatinized starch
- 210,000 35,000 210,000 35,000
- Manitol Mannitol
- 236,000 39,333 236,000 39,333
- Copovidona Copovidone
- 18,000 3,000 18,000 3,000
- Total (granulado) Total (granulated)
- 474,000 79,000 474,000 79,000
- Almidón pregelatinizado Pregelatinized starch
- 120,000 20,000 120,000 20,000
- Estearato de magnesio Magnesium stearate
- 6,000 1,000 6,000 1,000
- Total Total
- 600,000 100,000 600,000 100,000
20 Se disuelve copovidona en agua purificada a temperatura ambiente para producir un líquido de granulación. Un ingrediente activo de inhibidor de DPP IV con un grupo amino primario, manitol, almidón pregelatinizado y almidón de maíz se mezclan en un mezclador adecuado para producir la pre-mezcla. La pre-mezcla se humedece con el líquido de granulación y posteriormente se granula usando un 20 Copovidone is dissolved in purified water at room temperature to produce a granulation liquid. An active ingredient of DPP IV inhibitor with a primary amino group, mannitol, pregelatinized starch and corn starch are mixed in a suitable mixer to produce the pre-mix. The pre-mixture is moistened with the granulation liquid and subsequently granulated using a
25 mezclador de cizallamiento alto. El granulado húmedo se tamiza opcionalmente a través de un tamiz con un tamaño de malla de 1,6-3.0 mm. El granulado se seca a aproximadamente 600C en un secador de lecho fluido hasta que se obtiene una pérdida en el valor de secado de 2-4%. La Mezcla Final se comprime en núcleos de comprimidos. 25 high shear mixer. The wet granulate is optionally sieved through a sieve with a mesh size of 1.6-3.0 mm. The granulate is dried at approximately 600C in a fluid bed dryer until a loss in the drying value of 2-4% is obtained. The Final Mix is compressed into tablet cores.
Se suspenden en agua purificada en un mezclador adecuado, a temperatura They are suspended in purified water in a suitable mixer, at temperature
5 ambiente, hidroxipropilmetilcelulosa, polietilenglicol, talco, dióxido de titanio y óxido de hierro, para producir una suspensión de recubrimiento. Se recubren los núcleos de los comprimidos con la suspensión de recubrimiento hasta una ganancia de peso de aproximadamente 3% para producir comprimidos recubiertos de película. Pueden obtenerse las composiciones en comprimidos siguientes: 5 environment, hydroxypropyl methylcellulose, polyethylene glycol, talc, titanium dioxide and iron oxide, to produce a coating suspension. The cores of the tablets are coated with the coating suspension to a weight gain of approximately 3% to produce film-coated tablets. The following tablet compositions can be obtained:
10 10
- Componente Component
- mg mg mg mg mg mg mg mg mg mg
- Ingrediente activo Active ingredient
- 0,500 1,000 2,500 5,000 10,000 0.500 1,000 2,500 5,000 10,000
- Manitol Mannitol
- 67,450 66,950 65,450 130,900 125,900 67,450 66,950 65,450 130,900 125,900
- Almidón pregelatinizado Pregelatinized starch
- 9,000 9,000 9,000 18,000 18,000 9,000 9,000 9,000 18,000 18,000
- Almidón de maíz Cornstarch
- 9,000 9,000 9,000 18,000 18,000 9,000 9,000 9,000 18,000 18,000
- Copovidona Copovidone
- 2,700 2,700 2,700 5,400 5,400 2,700 2,700 2,700 5,400 5,400
- Estearato de magnesio Magnesium stearate
- 1,350 1,350 1,350 2,700 2,700 1,350 1,350 1,350 2,700 2,700
- Masa Total (núcleo del comprimido) Total Mass (tablet core)
- 90,000 90,000 90,000 180,000 180,000 90,000 90,000 90,000 180,000 180,000
- HPMC HPMC
- 1,500 1,500 1,500 2,500 2,500 1,500 1,500 1,500 2,500 2,500
- PEG PEG
- 0,150 0,150 0,150 0,250 0,250 0,150 0,150 0,150 0.250 0.250
- Dióxido de titanio Titanium dioxide
- 0,750 0,750 0,750 1,250 1,250 0.750 0.750 0.750 1,250 1,250
- Talco talcum powder
- 0,525 0,525 0,525 0,875 0,875 0.525 0.525 0.525 0.875 0.875
- Óxido de hierro amarillo Yellow iron oxide
- 0,075 0,075 0,075 0,125 0,125 0.075 0.075 0.075 0.125 0.125
- Masa Total (comprimido recubierto) Total Mass (coated tablet)
- 93,000 93,000 93,000 185,000 185,000 93,000 93,000 93,000 185,000 185,000
Se disuelve copovidona en agua purificada a temperatura ambiente para producir un líquido de granulación. Un ingrediente activo de inhibidor de DPP IV con 15 un grupo amino primario, manitol y almidón pregelatinizado se mezclan en un mezclador adecuado para producir una pre-mezcla. Se humedece la pre-mezcla con el Copovidone is dissolved in purified water at room temperature to produce a granulation liquid. An active ingredient of DPP IV inhibitor with a primary amino group, mannitol and pregelatinized starch is mixed in a suitable mixer to produce a pre-mix. The pre-mix is moistened with the
líquido de granulación y se granula posteriormente. El granulado húmedo se tamiza opcionalmente a través de un tamiz adecuado. El granulado se seca a aproximadamente 500C en un secador adecuado hasta que se obtiene una pérdida en el valor de secado de 3-5%. Se tamiza el granulado seco a través de un tamiz con un granulation liquid and subsequently granulated. The wet granulate is optionally sieved through a suitable sieve. The granulate is dried at approximately 500C in a suitable dryer until a loss in the drying value of 3-5% is obtained. Dry granulate is screened through a sieve with a
5 tamaño de malla de 1,0 mm. 5 mesh size of 1.0 mm.
El estearato de magnesio se pasa a través de un tamiz de 1,0 mm y se añade al granulado. Posteriormente, se produce la mezcla final por mezclado final en un mezclador adecuado y la mezcla final se comprime en comprimidos. Pueden obtenerse las composiciones en comprimidos siguientes: Magnesium stearate is passed through a 1.0 mm sieve and added to the granulate. Subsequently, the final mixture is produced by final mixing in a suitable mixer and the final mixture is compressed into tablets. The following tablet compositions can be obtained:
10 10
- Componente Component
- mg mg mg mg mg mg mg mg mg mg
- Ingrediente activo Active ingredient
- 0,500 1,000 2,500 5,000 10,000 0.500 1,000 2,500 5,000 10,000
- Manitol Mannitol
- 27,500 27,000 67,500 135,000 130,000 27,500 27,000 67,500 135,000 130,000
- Almidón pregelatinizado Pregelatinized starch
- 20,000 20,000 50,000 100,000 100,000 20,000 20,000 50,000 100,000 100,000
- Copovidona Copovidone
- 1,500 1,500 3,750 7,500 7,500 1,500 1,500 3,750 7,500 7,500
- Estearato de magnesio Magnesium stearate
- 0,500 0,500 1,250 2,500 2,500 0.500 0.500 1,250 2,500 2,500
- Masa total del comprimido Total tablet mass
- 50,000 50,000 125,000 250,000 250,000 50,000 50,000 125,000 250,000 250,000
Ejemplo 6 -Variantes de la formulación en comprimidos Se disuelve copovidona en agua purificada a temperatura ambiente para Example 6 - Variants of the tablet formulation Copovidone is dissolved in purified water at room temperature to
15 producir un líquido de granulación. Un ingrediente activo de inhibidor de DPP IV con un grupo amino primario y una parte de manitol, almidón pregelatinizado y almidón de maíz se mezclan en un mezclador adecuado, para producir una pre-mezcla. Se humedece la pre-mezcla con el líquido de granulación y se granula posteriormente. Se tamiza el granulado húmedo a través de un tamiz adecuado. El granulado se seca a 15 produce a granulation liquid. An active ingredient of DPP IV inhibitor with a primary amino group and a portion of mannitol, pregelatinized starch and corn starch are mixed in a suitable mixer, to produce a pre-mix. The pre-mixture is moistened with the granulation liquid and subsequently granulated. The wet granulate is screened through a suitable sieve. The granulate is dried to
20 aproximadamente 600C de temperatura del aire de entrada en un secador de lecho fluido hasta que se obtiene una pérdida en el valor de secado de 1-4%. Se tamiza el granulado seco a través de un tamiz con un tamaño de malla de 1,0 mm. Se hace pasar estearato de magnesio a través de un tamiz para deshacer los terrones y se añade al granulado. Adicionalmente, la parte restante de los excipientes Approximately 600C of inlet air temperature in a fluid bed dryer until a loss in the drying value of 1-4% is obtained. Dry granulate is screened through a sieve with a mesh size of 1.0 mm. Magnesium stearate is passed through a sieve to break the lumps and added to the granulate. Additionally, the remaining part of the excipients
25 se añade de manera extragranular en esta etapa del proceso. Posteriormente, se produce la mezcla final mezclando finalmente en un mezclador adecuado y comprimiendo en núcleos de comprimidos. 25 is added extragranularly at this stage of the process. Subsequently, the final mixture is produced by finally mixing in a suitable mixer and compressing into tablet cores.
Se suspenden en agua purificada en un mezclador adecuado, a temperatura ambiente, hidroxipropilmetilcelulosa, polietilenglicol, talco, dióxido de titanio y óxido de hierro, para producir una suspensión de recubrimiento. Se recubren los núcleos de los comprimidos con la suspensión de recubrimiento hasta una ganancia de peso de aproximadamente 3% para producir comprimidos recubiertos de película. Se pueden obtener las variantes de la formulación siguientes: They are suspended in purified water in a suitable mixer, at room temperature, hydroxypropyl methylcellulose, polyethylene glycol, talc, titanium dioxide and iron oxide, to produce a coating suspension. The cores of the tablets are coated with the coating suspension to a weight gain of approximately 3% to produce film-coated tablets. The following formulation variants can be obtained:
Ejemplo 6.1 -Variantes de formulación con excipientes extragranulares
Example 6.1 - Formulation variants with extragranular excipients
- Componente Component
- Formulación E Formulación F Formulation E Formulation F
- mg/Comprimido mg / tablet
- %/Comprimido mg/Comprimido %/Comprimido %/Compressed mg / tablet %/Compressed
- Ingrediente activo Active ingredient
- 1,000 1,111 1,000 1,111 1,000 1,111 1,000 1,111
- Manitol Mannitol
- 23,300 25,889 66,950 74,389 23,300 25,889 66,950 74,389
- Almidón pregelatinizado Pregelatinized starch
- 4,500 5,000 4,500 5,000 4,500 5,000 4,500 5,000
- Almidón de maíz Cornstarch
- 4,500 5,000 4,500 5,000 4,500 5,000 4,500 5,000
- Copovidona Copovidone
- 1,350 1,500 2,700 3,000 1,350 1,500 2,700 3,000
- Total (granulado) Total (granulated)
- 34,650 38,500 79,650 88,500 34,650 38,500 79,650 88,500
- Almidón de maíz Cornstarch
- 4,500 5,000 4,500 5,000 4,500 5,000 4,500 5,000
- Almidón pregelatinizado Pregelatinized starch
- 4,500 5,000 4,500 5,000 4,500 5,000 4,500 5,000
- Manitol Mannitol
- 45,000 50,000 45,000 50,000
- Estearato de magnesio Magnesium stearate
- 1,350 1,500 1,350 1,500 1,350 1,500 1,350 1,500
- Total (núcleo de comprimido) Total (tablet core)
- 90,000 100,000 90,000 100,000 90,000 100,000 90,000 100,000
Ejemplo 6.2 -Variantes de formulación con disgregante extragranular adicional
Example 6.2 - Formulation variants with additional extragranular disintegrant
- Componente Component
- mg mg mg mg mg mg mg mg mg mg
- Ingrediente activo Active ingredient
- 0,500 1,000 2,500 5,000 10,000 0.500 1,000 2,500 5,000 10,000
- Manitol Mannitol
- 67,450 66,950 65,450 130,900 125,900 67,450 66,950 65,450 130,900 125,900
- Almidón pregelatinizado Pregelatinized starch
- 9,000 9,000 9,000 18,000 18,000 9,000 9,000 9,000 18,000 18,000
- Almidón de maíz Cornstarch
- 9,000 9,000 9,000 18,000 18,000 9,000 9,000 9,000 18,000 18,000
- Copovidona Copovidone
- 2,700 2,700 2,700 5,400 5,400 2,700 2,700 2,700 5,400 5,400
- Masa Total (granulado) Total Mass (granulated)
- 88,650 88,650 88,650 177,300 177,300 88,650 88,650 88,650 177,300 177,300
- Estearato de magnesio Magnesium stearate
- 1,350 1,350 1,350 2,700 2,700 1,350 1,350 1,350 2,700 2,700
- Crospovidona Crospovidone
- 2,000 2,000 2,000 4,000 4,000 2,000 2,000 2,000 4,000 4,000
- Masa Total (núcleo del comprimido) Total Mass (tablet core)
- 92,000 92,000 92,000 184,000 184,000 92,000 92,000 92,000 184,000 184,000
- HPMC HPMC
- 1,500 1,500 1,500 2,500 2,500 1,500 1,500 1,500 2,500 2,500
- PEG PEG
- 0,150 0,150 0,150 0,250 0,250 0,150 0,150 0,150 0.250 0.250
- Dióxido de titanio Titanium dioxide
- 0,750 0,750 0,750 1,250 1,250 0.750 0.750 0.750 1,250 1,250
- Talco talcum powder
- 0,525 0,525 0,525 0,875 0,875 0.525 0.525 0.525 0.875 0.875
- Óxido de hierro amarillo Yellow iron oxide
- 0,075 0,075 0,075 0,125 0,125 0.075 0.075 0.075 0.125 0.125
- Masa Total (comprimido recubierto) Total Mass (coated tablet)
- 95,000 95,000 95,000 189,000 189,000 95,000 95,000 95,000 189,000 189,000
Claims (12)
- • •
- 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(R)-amino-piperidin-1-il)xantina, 1 - [(4-methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8- (3- (R) -amino-piperidin-1-yl) xanthine,
- • •
- 1-[([1,5]naftiridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, 1 - [([1,5] naphthyridin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl ) xanthine,
- • •
- 1-[(Quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, 1 - [(Quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine,
- • •
- 2-((R)-3-Amino-piperidin-1-il)-3-(but-2-inil)-5-(4-metil-quinazolin-2-ilmetil)-3,5dihidro-imidazo[4,5-d]piridazin-4-ona, 2 - ((R) -3-Amino-piperidin-1-yl) -3- (but-2-inyl) -5- (4-methyl-quinazolin-2-ylmethyl) -3,5-dihydro-imidazo [4, 5-d] pyridazin-4-one,
- • •
- 1-[(4-Metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(2-amino-2-metil-propil)metilamino]-xantina, 1 - [(4-Methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - [(2-amino-2-methyl-propyl) methylamino] - xanthine,
- • •
- 1-[(3-Ciano-quinolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, 1 - [(3-Cyano-quinolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine,
- • •
- 1-(2-Ciano-bencil)-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)-xantina, 1- (2-Cyano-benzyl) -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) -xanthine,
- • •
- 1-[(4-Metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(S)-(2-aminopropil)metilamino]-xantina, 1 - [(4-Methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - [(S) - (2-aminopropyl) methylamino] -xanthine,
- • •
- 1-[(3-Ciano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, 1 - [(3-Cyano-pyridin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine,
- • •
- 1-[(4-Metil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, 1 - [(4-Methyl-pyrimidin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine,
- • •
- 1-[(4,6-Dimetil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1il)-xantina, y 1 - [(4,6-Dimethyl-pyrimidin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1il) -xanthine, and
- • •
- 1-[(Quinoxalin-6-il)metil]-3-metil-7-(2-butin-1-il)-8-((R)-3-amino-piperidin-1-il)xantina, 1 - [(Quinoxalin-6-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8 - ((R) -3-amino-piperidin-1-yl) xanthine,
- a. to.
- disolver el aglutinante en un disolvente para producir un líquido de granulación; dissolve the binder in a solvent to produce a granulation liquid;
- b. b.
- mezclar el inhibidor de DPP-IV, los diluyentes y el disgregante para producir una pre-mezcla; mix the DPP-IV inhibitor, diluents and disintegrant to produce a pre-mix;
- c. C.
- humedecer la pre-mezcla con el líquido de granulación y posteriormente granular la pre-mezcla humedecida; moisten the pre-mix with the granulation liquid and then granulate the moistened pre-mix;
- d. d.
- opcionalmente tamizar la pre-mezcla granulada a través de un tamiz con un tamaño de malla de al menos 1,0 mm; optionally sifting the granulated pre-mix through a screen with a mesh size of at least 1.0 mm;
- e.and.
- secar el granulado a aproximadamente 40-750C hasta que se obtiene la pérdida deseada en el valor de secado en el intervalo de 1-5%; Dry the granulate at approximately 40-750C until the desired loss in the drying value in the range of 1-5% is obtained;
- f. F.
- tamizar el granulado secado a través de un tamiz con un tamaño de malla de al menos 0,6 mm; sift the dried granulate through a sieve with a mesh size of at least 0.6 mm;
- g. g.
- añadir el lubricante al granulado para el mezclado final. add the lubricant to the granulate for final mixing.
- h. h.
- comprimir la mezcla final en núcleos de comprimidos; compress the final mixture into tablet cores;
- i. i.
- preparar una suspensión de recubrimiento; prepare a coating suspension;
- j. j.
- recubrir los núcleos de los comprimidos con la suspensión de recubrimiento hasta una ganancia de peso de aproximadamente 2-4 % para producir comprimidos recubiertos con película. coating the tablet cores with the coating suspension to a weight gain of approximately 2-4% to produce film-coated tablets.
- 10. 10.
- El proceso según la reivindicación 8, en el que parte de los excipientes se añaden de manera extragranular antes del mezclado final de la etapa g. The process according to claim 8, wherein part of the excipients are added extragranularly before the final mixing of step g.
- 11. eleven.
- El proceso según la reivindicación 8, en el que el granulado producido en las etapas a-e se produce en un proceso de granulación de cizallamiento alto en un solo recipiente y posteriormente se seca en un granulador con un solo recipiente. The process according to claim 8, wherein the granulate produced in steps a-e is produced in a high shear granulation process in a single container and subsequently dried in a granulator with a single container.
- 12. 12.
- Una forma de dosificación preparada con la composición farmacéutica según la reivindicación 1, que contiene el ingrediente activo en una dosificación de 0,5 mg, 1 mg, 2,5 mg, 5 mg ó 10 mg. A dosage form prepared with the pharmaceutical composition according to claim 1, containing the active ingredient in a dosage of 0.5 mg, 1 mg, 2.5 mg, 5 mg or 10 mg.
- 13. 13.
- La composición farmacéutica según la reivindicación 1, en la que el inhibidor de DPP IV es 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(R)amino-piperidin-1-il)-xantina. The pharmaceutical composition according to claim 1, wherein the DPP IV inhibitor is 1 - [(4-methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) - 8- (3- (R) amino-piperidin-1-yl) -xanthine.
- 14. 14.
- El proceso según la reivindicación 8 ó 9, en el que el inhibidor de DPP IV es 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(R)-amino-piperidin-1il)-xantina. The process according to claim 8 or 9, wherein the DPP IV inhibitor is 1 - [(4-methyl-quinazolin-2-yl) methyl] -3-methyl-7- (2-butin-1-yl) -8- (3- (R) -amino-piperidin-1-yl) -xanthine.
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EP06009201A EP1852108A1 (en) | 2006-05-04 | 2006-05-04 | DPP IV inhibitor formulations |
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ES10175188.1T Active ES2538818T3 (en) | 2006-05-04 | 2007-04-30 | DPP IV inhibitor formulations |
ES10175638T Active ES2527409T4 (en) | 2006-05-04 | 2007-04-30 | DPP IV inhibitor formulations |
ES07728658T Active ES2348576T3 (en) | 2006-05-04 | 2007-04-30 | DPP INHIBITOR FORMULATIONS IV. |
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ES10175188.1T Active ES2538818T3 (en) | 2006-05-04 | 2007-04-30 | DPP IV inhibitor formulations |
ES10175638T Active ES2527409T4 (en) | 2006-05-04 | 2007-04-30 | DPP IV inhibitor formulations |
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Families Citing this family (115)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
US7495005B2 (en) * | 2002-08-22 | 2009-02-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, their preparation and their use in pharmaceutical compositions |
US7482337B2 (en) * | 2002-11-08 | 2009-01-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions |
US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
US7439370B2 (en) | 2004-05-10 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides |
DE102004030502A1 (en) | 2004-06-24 | 2006-01-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel imidazoles and triazoles, their preparation and use as medicines |
DE102004054054A1 (en) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Process for preparing chiral 8- (3-amino-piperidin-1-yl) -xanthines |
US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
DE102005035891A1 (en) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8- (3-amino-piperidin-1-yl) -xanthines, their preparation and their use as pharmaceuticals |
EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
PE20110235A1 (en) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | PHARMACEUTICAL COMBINATIONS INCLUDING LINAGLIPTIN AND METMORPHINE |
EA030606B1 (en) | 2006-05-04 | 2018-08-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Methods of preparing a medicament comprising polymorphs |
JP5453086B2 (en) | 2006-06-06 | 2014-03-26 | イントラ−セルラー・セラピーズ・インコーポレイテッド | Organic compounds |
US8071583B2 (en) | 2006-08-08 | 2011-12-06 | Boehringer Ingelheim International Gmbh | Pyrrolo[3,2-D] pyrimidines as DPP-IV inhibitors for the treatment of diabetes mellitus |
EP2025674A1 (en) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituted tetra hydro naphthalines, method for their manufacture and their use as drugs |
PE20090938A1 (en) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | PHARMACEUTICAL COMPOSITION INCLUDING A BENZENE DERIVATIVE SUBSTITUTED WITH GLUCOPYRANOSIL |
US8846693B2 (en) | 2007-12-06 | 2014-09-30 | Intra-Cellular Therapies, Inc. | Optionally substituted pyrazolo[3,4-d]pyrimidine-4,6-diones |
PE20091730A1 (en) * | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | FORMULATIONS INVOLVING A DPP4 INHIBITOR |
UY32030A (en) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "TREATMENT FOR DIABETES IN INAPPROPRIATE PATIENTS FOR THERAPY WITH METFORMIN" |
KR20200118243A (en) | 2008-08-06 | 2020-10-14 | 베링거 인겔하임 인터내셔날 게엠베하 | Treatment for diabetes in patients inappropriate for metformin therapy |
CA2733778A1 (en) * | 2008-08-14 | 2010-02-18 | Hiroshi Uchida | Stabilized pharmaceutical composition |
PE20110297A1 (en) | 2008-08-15 | 2011-05-26 | Boehringer Ingelheim Int | DPP-4 INHIBITORS FOR WOUND HEALING |
KR20110067096A (en) | 2008-09-10 | 2011-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | Combination therapy for the treatment of diabetes and related conditions |
JP5694773B2 (en) * | 2008-09-30 | 2015-04-01 | テバ製薬株式会社 | COMPRESSION MOLDED PREPARATION AND METHOD |
US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
GEP20146046B (en) | 2008-12-06 | 2014-02-25 | Intracellular Therapies Inc | Organic compounds |
MA32940B1 (en) | 2008-12-06 | 2012-01-02 | Intra Cellular Therapies Inc | ORGANIC COMPOUNDS |
EP2367428B1 (en) | 2008-12-06 | 2016-04-06 | Intra-Cellular Therapies, Inc. | Organic compounds |
JP2012512848A (en) | 2008-12-23 | 2012-06-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Salt forms of organic compounds |
US8404727B2 (en) | 2009-01-07 | 2013-03-26 | Glenmark Pharmaceuticals S.A. | Pharmaceutical composition that includes a dipeptidyl peptidase-IV inhibitor |
AR074990A1 (en) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | TREATMENT OF DIABETES IN PATIENTS WITH AN INAPPROPRIATE GLUCEMIC CONTROL THROUGH METFORMIN THERAPY |
TWI466672B (en) | 2009-01-29 | 2015-01-01 | Boehringer Ingelheim Int | Treatment for diabetes in paediatric patients |
WO2010092125A1 (en) * | 2009-02-13 | 2010-08-19 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof |
UY32427A (en) * | 2009-02-13 | 2010-09-30 | Boheringer Ingelheim Internat Gmbh | PHARMACEUTICAL COMPOSITION, PHARMACEUTICAL FORM, PROCEDURE FOR PREPARATION, METHODS OF TREATMENT AND USES OF THE SAME |
NZ594044A (en) * | 2009-02-13 | 2014-08-29 | Boehringer Ingelheim Int | Antidiabetic medications comprising a dpp-4 inhibitor (linagliptin) optionally in combination with other antidiabetics |
MX2011008554A (en) | 2009-05-19 | 2011-10-06 | Celgene Corp | Formulations of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1 ,3-dione. |
EP2483286B1 (en) | 2009-09-30 | 2016-07-13 | Boehringer Ingelheim International GmbH | Method for the preparation of a crystalline form of 1-chloro-4-(beta-d-glucopyranos-1-yl)-2-(4-((s)-tetrahydrofuran-3-yloxy)benzyl)benzene |
PT2486029E (en) | 2009-09-30 | 2015-10-14 | Boehringer Ingelheim Int | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives |
CN102596191B (en) | 2009-10-02 | 2016-12-21 | 勃林格殷格翰国际有限公司 | Comprise the pharmaceutical composition of BI 1356 and metformin |
UY32919A (en) | 2009-10-02 | 2011-04-29 | Boehringer Ingelheim Int | Pharmaceutical composition, pharmaceutical dosage form, procedure for its preparation, methods for its treatment and its uses |
BR112012012641A2 (en) | 2009-11-27 | 2020-08-11 | Boehringer Ingelheim International Gmbh | TREATMENT OF GENOTYPED DIABETIC PATIENTS WITH DPP-lVTAL INHIBITORS LIKE LINAGLIPTIN |
JP5775463B2 (en) * | 2009-12-18 | 2015-09-09 | 田辺三菱製薬株式会社 | Elution stability formulation |
WO2011107494A1 (en) | 2010-03-03 | 2011-09-09 | Sanofi | Novel aromatic glycoside derivatives, medicaments containing said compounds, and the use thereof |
JP5031054B2 (en) * | 2010-03-18 | 2012-09-19 | 信越化学工業株式会社 | Low substituted hydroxypropyl cellulose and solid preparation containing the same |
WO2011113947A1 (en) | 2010-03-18 | 2011-09-22 | Boehringer Ingelheim International Gmbh | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
WO2011138421A1 (en) | 2010-05-05 | 2011-11-10 | Boehringer Ingelheim International Gmbh | Combination therapy |
CN102883711A (en) * | 2010-05-05 | 2013-01-16 | 贝林格尔.英格海姆国际有限公司 | Pharmaceutical formulations comprising pioglitazone and linagliptin |
JP5879336B2 (en) | 2010-05-31 | 2016-03-08 | イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. | Organic compounds |
EP2590657A4 (en) | 2010-05-31 | 2014-02-12 | Intra Cellular Therapies Inc | Organic compounds |
WO2011157827A1 (en) | 2010-06-18 | 2011-12-22 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
EP3366304B1 (en) | 2010-06-24 | 2020-05-13 | Boehringer Ingelheim International GmbH | Diabetes therapy |
TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
AR085689A1 (en) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | PHARMACEUTICAL COMPOSITIONS OF METFORMIN, LINAGLIPTINE AND AN SGLT-2 INHIBITOR |
US8871758B2 (en) | 2011-03-08 | 2014-10-28 | Sanofi | Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
WO2012120054A1 (en) | 2011-03-08 | 2012-09-13 | Sanofi | Di- and tri-substituted oxathiazine derivates, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
WO2012120052A1 (en) | 2011-03-08 | 2012-09-13 | Sanofi | Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof |
US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
EP2683699B1 (en) | 2011-03-08 | 2015-06-24 | Sanofi | Di- and tri-substituted oxathiazine derivates, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
JP6028016B2 (en) | 2011-05-10 | 2016-11-16 | サンド・アクチエンゲゼルシヤフト | Polymorphs of linagliptin benzoate |
WO2012170702A1 (en) | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
WO2013010964A1 (en) | 2011-07-15 | 2013-01-24 | Boehringer Ingelheim International Gmbh | Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions |
WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
US20130172244A1 (en) | 2011-12-29 | 2013-07-04 | Thomas Klein | Subcutaneous therapeutic use of dpp-4 inhibitor |
US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
US9192617B2 (en) | 2012-03-20 | 2015-11-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
WO2013171167A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
US20130303554A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in sirs and/or sepsis |
WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
EP2854812A1 (en) | 2012-05-24 | 2015-04-08 | Boehringer Ingelheim International GmbH | A xanthine derivative as dpp -4 inhibitor for use in the treatment of autoimmune diabetes, particularly lada |
WO2013174769A1 (en) | 2012-05-25 | 2013-11-28 | Boehringer Ingelheim International Gmbh | Use of keratinocytes as a biologically active substance in the treatment of wounds, such as diabetic wounds, optionally in combination with a dpp-4 inhibitor |
CN104519874B (en) | 2012-06-05 | 2018-08-03 | 武田药品工业株式会社 | Solid pharmaceutical preparation |
JP6215940B2 (en) | 2012-08-13 | 2017-10-18 | サンド・アクチエンゲゼルシヤフト | 8-[(3R) -3-Amino-1-piperidinyl] -7- (2-butyn-1-yl) -3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl) Stable pharmaceutical composition comprising methyl] -1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof |
WO2014045266A1 (en) | 2012-09-24 | 2014-03-27 | Ulf Eriksson | Treatment of type 2 diabetes and related conditions |
WO2014051023A1 (en) * | 2012-09-27 | 2014-04-03 | 株式会社 三和化学研究所 | Anagliptin-containing preparation |
WO2014051025A1 (en) * | 2012-09-27 | 2014-04-03 | 株式会社 三和化学研究所 | Anagliptin-containing solid preparation |
JP6283313B2 (en) * | 2012-09-27 | 2018-02-21 | 株式会社三和化学研究所 | Anagliptin-containing pharmaceutical composition |
WO2014064215A1 (en) | 2012-10-24 | 2014-05-01 | INSERM (Institut National de la Santé et de la Recherche Médicale) | TPL2 KINASE INHIBITORS FOR PREVENTING OR TREATING DIABETES AND FOR PROMOTING β-CELL SURVIVAL |
JP6283316B2 (en) * | 2012-10-26 | 2018-02-21 | 株式会社三和化学研究所 | Anagliptin-containing solid preparation |
WO2014080384A1 (en) | 2012-11-26 | 2014-05-30 | Ranbaxy Laboratories Limited | Pharmaceutical composition of linagliptin |
CN110075098A (en) | 2013-03-15 | 2019-08-02 | 勃林格殷格翰国际有限公司 | Purposes of the Li Gelieting in heart and protection renal antidiabetic treatment |
US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
US20140303097A1 (en) | 2013-04-05 | 2014-10-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
ES2702174T3 (en) | 2013-04-05 | 2019-02-27 | Boehringer Ingelheim Int | Therapeutic uses of empagliflozin |
EA033286B1 (en) | 2013-04-18 | 2019-09-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Method of treating or delaying the progression of chronic kidney disease |
TR201310724A2 (en) | 2013-09-12 | 2015-03-23 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Pharmaceutical formulati̇ons of linagliptin |
EP2848241A1 (en) | 2013-09-12 | 2015-03-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Effervescent formulations of linagliptin |
EP2848242A1 (en) | 2013-09-12 | 2015-03-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Orally disintegrating formulations of Linagliptin |
WO2015110962A1 (en) | 2014-01-21 | 2015-07-30 | Wockhardt Limited | Solid oral pharmaceutical compositions comprising fixed dose combination of metformin and linagliptin or salts thereof |
ES2950384T3 (en) | 2014-02-28 | 2023-10-09 | Boehringer Ingelheim Int | Medical use of a DPP-4 inhibitor |
US20150283248A1 (en) * | 2014-04-02 | 2015-10-08 | Aurobindo Pharma Ltd. | Pharmaceutical compositions of Linagliptin and process for preparation thereof |
US9546175B2 (en) | 2014-08-07 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Organic compounds |
CN105878349A (en) * | 2014-11-28 | 2016-08-24 | 于凯 | Composition for preventing and treating osteoporosis caused by diabetics |
US10426818B2 (en) | 2015-03-24 | 2019-10-01 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Method and pharmaceutical composition for use in the treatment of diabetes |
EP3310357A1 (en) * | 2015-06-17 | 2018-04-25 | H e x a l Aktiengesellschaft | Alogliptin formulation |
EA037498B1 (en) | 2015-10-09 | 2021-04-05 | Хексаль Аг | Pharmaceutical composition containing 8-[(3r)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[4-methyl-2-quinazolinyl)methyl]-1h-purine-2,6-dione or a pharmaceutically acceptable salt thereof |
EP3156048A1 (en) | 2015-10-13 | 2017-04-19 | Galenicum Health S.L. | Stable pharmaceutical composition of linagliptin in the form of immediate release tablets |
US9727330B2 (en) * | 2015-11-25 | 2017-08-08 | Red Hat, Inc. | Source to image transformation pipeline for a platform-as-a-service system |
CN105853382B (en) * | 2016-05-19 | 2019-07-19 | 广州迈达康医药科技有限公司 | A kind of Li Gelieting oral disintegrating tablet and preparation method thereof |
EP3468562A1 (en) | 2016-06-10 | 2019-04-17 | Boehringer Ingelheim International GmbH | Combinations of linagliptin and metformin |
CN106236754A (en) * | 2016-07-31 | 2016-12-21 | 合肥远志医药科技开发有限公司 | A kind of compositions comprising Li Gelieting active component and preparation method thereof |
CN106137991A (en) * | 2016-08-01 | 2016-11-23 | 合肥远志医药科技开发有限公司 | A kind of Li Gelieting sheet method of granulating |
EP3551202B1 (en) | 2016-12-06 | 2024-01-24 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of enhancing the potency of incretin-based drugs in subjects in need thereof |
WO2020009675A2 (en) * | 2018-06-01 | 2020-01-09 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Solid oral pharmaceutical compositions of linagliptin |
JP2022504333A (en) * | 2018-10-05 | 2022-01-13 | アイエスピー インヴェストメンツ エルエルシー | Smooth high solid content film coating composition containing water-soluble cellulose ether, its preparation method and its usage method |
EP4045048A4 (en) | 2019-10-14 | 2023-05-24 | Santa Farma Ilaç Sanayi A.S. | Oral formulations comprising sitagliptin hci monohydrate with improved pharmaceutical characteristics |
WO2021109970A1 (en) * | 2019-12-02 | 2021-06-10 | 成都苑东生物制药股份有限公司 | Xanthine derivative pharmaceutical composition and preparation method therefor |
CN117858703A (en) | 2021-07-22 | 2024-04-09 | 新梅斯托克公司 | Method for preparing pharmaceutical composition comprising linagliptin and metformin hydrochloride |
KR20230126664A (en) | 2022-02-23 | 2023-08-30 | 주식회사 제뉴원사이언스 | Pharmaceutical combination of controlled drug delivery comprising linagliptin or a pharmaceutically acceptable salt thereof and metformin or a pharmaceutically acceptable salt thereof |
CN115227661B (en) * | 2022-09-22 | 2022-12-13 | 北京惠之衡生物科技有限公司 | Linagliptin tablet and preparation method thereof |
WO2024091863A1 (en) | 2022-10-25 | 2024-05-02 | Starrock Pharma Llc | Combinatorial, and rotational combinatorial therapies for obesity and other diseases |
Family Cites Families (472)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2056046A (en) * | 1933-05-19 | 1936-09-29 | Rhone Poulenc Sa | Manufacture of bases derived from benz-dioxane |
US2375138A (en) * | 1942-05-01 | 1945-05-01 | American Cyanamid Co | Alkamine esters of aryloxymethyl benzoic acid |
US2629736A (en) * | 1951-02-24 | 1953-02-24 | Searle & Co | Basically substituted n-alkyl derivatives of alpha, beta, beta-triarylpropionamides |
US2730544A (en) * | 1952-07-23 | 1956-01-10 | Sahyun Lab | Alkylaminoalkyl esters of hydroxycyclohexylbenzoic acid |
US2750387A (en) * | 1953-11-25 | 1956-06-12 | Searle & Co | Basically substituted derivatives of diarylaminobenzamides |
DE1211359B (en) * | 1955-11-29 | 1966-02-24 | Oreal | Oxidant-free cold dye for human hair |
US2928833A (en) * | 1959-03-03 | 1960-03-15 | S E Massengill Company | Theophylline derivatives |
US3174901A (en) * | 1963-01-31 | 1965-03-23 | Jan Marcel Didier Aron Samuel | Process for the oral treatment of diabetes |
US3454635A (en) * | 1965-07-27 | 1969-07-08 | Hoechst Ag | Benzenesulfonyl-ureas and process for their manufacture |
US3673241A (en) * | 1968-04-04 | 1972-06-27 | Ciba Geigy Corp | Substituted benzaldehyde guanylhydrazones |
ES385302A1 (en) | 1970-10-22 | 1973-04-16 | Miquel S A Lab | Procedure for the obtaining of trisused derivatives of etilendiamine. (Machine-translation by Google Translate, not legally binding) |
DE2205815A1 (en) | 1972-02-08 | 1973-08-16 | Hoechst Ag | N-(oxazolin-2-yl)-piperazine - with antitussive activity |
JPS5512435B2 (en) * | 1972-07-01 | 1980-04-02 | ||
US4005208A (en) * | 1975-05-16 | 1977-01-25 | Smithkline Corporation | N-Heterocyclic-9-xanthenylamines |
US4061753A (en) | 1976-02-06 | 1977-12-06 | Interx Research Corporation | Treating psoriasis with transient pro-drug forms of xanthine derivatives |
AU508480B2 (en) | 1977-04-13 | 1980-03-20 | Asahi Kasei Kogyo Kabushiki Kaisha | Microcrystalline cellulose excipient and pharmaceutical composition containing thesame |
NO154918C (en) | 1977-08-27 | 1987-01-14 | Bayer Ag | ANALOGUE PROCEDURE FOR THE PREPARATION OF THERAPEUTIC ACTIVE DERIVATIVES OF 3,4,5-TRIHYDROXYPIPERIDINE. |
DE2758025A1 (en) | 1977-12-24 | 1979-07-12 | Bayer Ag | Tri:hydroxy-piperidine derivs. - useful as glucosidase inhibitors for treating diabetes etc. and as animal feed additives |
DE2929596A1 (en) | 1979-07-21 | 1981-02-05 | Hoechst Ag | METHOD FOR PRODUCING OXOALKYL XANTHINES |
CY1306A (en) | 1980-10-01 | 1985-12-06 | Glaxo Group Ltd | Aminoalkyl furan derivative |
US4382091A (en) | 1981-04-30 | 1983-05-03 | Syntex (U.S.A.) Inc. | Stabilization of 1-substituted imidazole derivatives in talc |
FR2558162B1 (en) * | 1984-01-17 | 1986-04-25 | Adir | NOVEL XANTHINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
FI79107C (en) * | 1984-06-25 | 1989-11-10 | Orion Yhtymae Oy | Process for the preparation of stable form of prazosin hydrochloride. |
JPS6130567A (en) | 1984-07-23 | 1986-02-12 | Shiseido Co Ltd | Method of stabilizing urea |
JPS61124383A (en) | 1984-11-16 | 1986-06-12 | Unitika Ltd | Stabilization of immobilized fibrinolytic enzyme |
AR240698A1 (en) * | 1985-01-19 | 1990-09-28 | Takeda Chemical Industries Ltd | Process for the preparation of 5-(4-(2-(5-ethyl-2-pyridil)-ethoxy)benzyl)-2,4-thiazolodinedione and their salts |
CA1242699A (en) | 1985-02-01 | 1988-10-04 | Bristol-Myers Company | Cefbuperazone and derivatives thereof |
GB8515934D0 (en) * | 1985-06-24 | 1985-07-24 | Janssen Pharmaceutica Nv | (4-piperidinomethyl and-hetero)purines |
US5258380A (en) * | 1985-06-24 | 1993-11-02 | Janssen Pharmaceutica N.V. | (4-piperidinylmethyl and -hetero)purines |
ES2058061T3 (en) | 1985-10-25 | 1994-11-01 | Beecham Group Plc | DERIVED FROM PIPERIDINE, ITS PREPARATION AND ITS USE AS A MEDICINAL PRODUCT. |
US5034225A (en) | 1985-12-17 | 1991-07-23 | Genentech Inc. | Stabilized human tissue plasminogen activator compositions |
US5433959A (en) | 1986-02-13 | 1995-07-18 | Takeda Chemical Industries, Ltd. | Stabilized pharmaceutical composition |
EP0237608B1 (en) | 1986-03-21 | 1992-01-29 | HEUMANN PHARMA GMBH & CO | Crystalline anhydrous sigma-form of 2-[4-(2-furoyl-(2-piperazin)-1-yl]-4-amino-6,7-dimethoxyquinazoline hydrochloride, and process for its preparation |
US5120712A (en) | 1986-05-05 | 1992-06-09 | The General Hospital Corporation | Insulinotropic hormone |
ATE110083T1 (en) | 1986-05-05 | 1994-09-15 | Gen Hospital Corp | INSULINOTROPIC HORMONE. |
AU619444B2 (en) | 1986-06-02 | 1992-01-30 | Nippon Chemiphar Co. Ltd. | 2-(2-aminobenzylsulfinyl)- benzimidazole derivatives |
US4968672A (en) | 1987-01-02 | 1990-11-06 | The United States Of America As Represented By The Department Of Health And Human Services | Adenosine receptor prodrugs |
US4743450A (en) | 1987-02-24 | 1988-05-10 | Warner-Lambert Company | Stabilized compositions |
JPS6440433A (en) | 1987-08-05 | 1989-02-10 | Green Cross Corp | Aqueous liquid composition of thrombin |
DE68920773T2 (en) | 1988-05-19 | 1995-05-18 | Chugai Pharmaceutical Co Ltd | Quinolonecarboxylic acid derivatives. |
US5329025A (en) * | 1988-09-21 | 1994-07-12 | G. D. Searle & Co. | 3-azido compound |
DE3926119A1 (en) | 1989-08-08 | 1991-02-14 | Bayer Ag | 3-AMINO-5-AMINOCARBONYL-1,2,4-TRIAZOLE DERIVATIVES |
US5234897A (en) * | 1989-03-15 | 1993-08-10 | Bayer Aktiengesellschaft | Herbicidal 3-amino-5-aminocarbonyl-1,2,4-triazoles |
GB8906792D0 (en) | 1989-03-23 | 1989-05-10 | Beecham Wuelfing Gmbh & Co Kg | Treatment and compounds |
DE3916430A1 (en) | 1989-05-20 | 1990-11-22 | Bayer Ag | METHOD FOR PRODUCING 3-AMINO-5-AMINOCARBONYL-1,2,4-TRIAZOLE DERIVATIVES |
IL94390A (en) | 1989-05-30 | 1996-03-31 | Merck & Co Inc | Di-substituted imidazo fused 6-membered nitrogen-containing heterocycles and pharmaceutical compositions containing them |
US5332744A (en) * | 1989-05-30 | 1994-07-26 | Merck & Co., Inc. | Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists |
US5223499A (en) * | 1989-05-30 | 1993-06-29 | Merck & Co., Inc. | 6-amino substituted imidazo[4,5-bipyridines as angiotensin II antagonists |
FI94339C (en) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Process for the preparation of pharmaceutically acceptable [R- (R *, R *)] - 2- (4-fluorophenyl) -, - dihydroxy-5- (1-methylethyl) -3-phenyl-4 - [(phenylamino) carbonyl] -1H- for the preparation of pyrrole-1-heptanoic acid and its pharmaceutically acceptable salts |
HU208115B (en) | 1989-10-03 | 1993-08-30 | Biochemie Gmbh | New process for producting pleuromutilin derivatives |
FR2654935B1 (en) * | 1989-11-28 | 1994-07-01 | Lvmh Rech | USE OF XANTHINES, WHICH MAY BE INCORPORATED IN LIPOSOMES, TO PROMOTE PIGMENTATION OF THE SKIN OR HAIR. |
DE122007000050I1 (en) | 1990-02-19 | 2007-11-08 | Novartis Ag | acyl compounds |
KR930000861B1 (en) | 1990-02-27 | 1993-02-08 | 한미약품공업 주식회사 | Omeprazole rectal composition |
DE69104453T2 (en) | 1990-09-13 | 1995-03-16 | Akzo Nv | Stabilized solid chemical compositions. |
GB9020959D0 (en) | 1990-09-26 | 1990-11-07 | Beecham Group Plc | Novel compounds |
US5084460A (en) * | 1990-12-24 | 1992-01-28 | A. H. Robins Company, Incorporated | Methods of therapeutic treatment with N-(3-ouinuclidinyl)-2-hydroxybenzamides and thiobenzamides |
US5602127A (en) | 1991-02-06 | 1997-02-11 | Karl Thomae Gmbh | (Alkanesultam-1-yl)-benzimidazol-1-yl)-1yl)-methyl-biphenyls useful as angiotensin-II antagonists |
US5594003A (en) | 1991-02-06 | 1997-01-14 | Dr. Karl Thomae Gmbh | Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biphenyls useful as angiotensin-II antagonists |
US5591762A (en) | 1991-02-06 | 1997-01-07 | Dr. Karl Thomae Gmbh | Benzimidazoles useful as angiotensin-11 antagonists |
GB9109862D0 (en) | 1991-05-08 | 1991-07-03 | Beecham Lab Sa | Pharmaceutical formulations |
DE4124150A1 (en) * | 1991-07-20 | 1993-01-21 | Bayer Ag | SUBSTITUTED TRIAZOLES |
US5300298A (en) * | 1992-05-06 | 1994-04-05 | The Pennsylvania Research Corporation | Methods of treating obesity with purine related compounds |
GB9215633D0 (en) | 1992-07-23 | 1992-09-09 | Smithkline Beecham Plc | Novel treatment |
TW307769B (en) | 1992-07-31 | 1997-06-11 | Shionogi & Co | |
TW252044B (en) | 1992-08-10 | 1995-07-21 | Boehringer Ingelheim Kg | |
US5358941A (en) | 1992-12-02 | 1994-10-25 | Merck & Co., Inc. | Dry mix formulation for bisphosphonic acids with lactose |
DE4242459A1 (en) * | 1992-12-16 | 1994-06-23 | Merck Patent Gmbh | imidazopyridines |
AU6087894A (en) | 1993-01-14 | 1994-08-15 | Cell Therapeutics, Inc. | Acetal or ketal substituted therapeutic compounds |
CA2118117A1 (en) | 1993-02-18 | 1994-08-19 | Shigeki Fujiwara | Adenosine uptake inhibitor |
JP3726291B2 (en) | 1993-07-05 | 2005-12-14 | 三菱ウェルファーマ株式会社 | Benzoxazine compound having stable crystal structure and process for producing the same |
FR2707641B1 (en) | 1993-07-16 | 1995-08-25 | Fournier Ind & Sante | Compounds of imidazol-5-carboxamide, their process for preparing their intermediates and their use in therapy. |
DE4339868A1 (en) | 1993-11-23 | 1995-05-24 | Merck Patent Gmbh | imidazopyridazines |
DE4404183A1 (en) | 1994-02-10 | 1995-08-17 | Merck Patent Gmbh | 4-amino-1-piperidylbenzoylguanidine |
US5545745A (en) | 1994-05-23 | 1996-08-13 | Sepracor, Inc. | Enantioselective preparation of optically pure albuterol |
CO4410190A1 (en) | 1994-09-19 | 1997-01-09 | Lilly Co Eli | 3- [4- (2-AMINOETOXI) -BENZOIL] -2-ARIL-6-HYDROXYBENZO [b] CRYSTALLINE THIOPHEN |
AU699489B2 (en) | 1994-10-12 | 1998-12-03 | Euro-Celtique S.A. | Novel benzoxazoles |
GB9501178D0 (en) | 1995-01-20 | 1995-03-08 | Wellcome Found | Guanine derivative |
JPH11505241A (en) | 1995-05-19 | 1999-05-18 | カイロサイエンス・リミテッド | Xanthines and their therapeutic use |
JPH08333339A (en) | 1995-06-08 | 1996-12-17 | Fujisawa Pharmaceut Co Ltd | Production of optically active piperidineacetic acid derivative |
GB9523752D0 (en) | 1995-11-21 | 1996-01-24 | Pfizer Ltd | Pharmaceutical formulations |
DE19543478A1 (en) | 1995-11-22 | 1997-05-28 | Bayer Ag | Crystalline hydrochloride of {(R) - (-) - 2N- [4- (1,1-dioxido-3-oxo-2,3-dihydrobenzisothiazol-2-yl) -buytl] aminomethyl} -chroman |
FR2742751B1 (en) | 1995-12-22 | 1998-01-30 | Rhone Poulenc Rorer Sa | NOVEL TAXOIDS, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
CA2241746A1 (en) | 1995-12-26 | 1997-07-03 | Alteon Inc. | N-acylaminoalkylhydrazinecarboximidamides |
US5891855A (en) | 1996-02-12 | 1999-04-06 | The Scripps Research Institute | Inhibitors of leaderless protein export |
DE19616486C5 (en) * | 1996-04-25 | 2016-06-30 | Royalty Pharma Collection Trust | Method for lowering the blood glucose level in mammals |
TW518219B (en) | 1996-04-26 | 2003-01-21 | Chugai Pharmaceutical Co Ltd | Erythropoietin solution preparation |
US5965555A (en) | 1996-06-07 | 1999-10-12 | Hoechst Aktiengesellschaft | Xanthine compounds having terminally animated alkynol side chains |
WO1997046526A1 (en) | 1996-06-07 | 1997-12-11 | Eisai Co., Ltd. | Stable polymorphs of donepezil (1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine) hydrochloride and process for production |
US5958951A (en) | 1996-06-14 | 1999-09-28 | Novo Nordiskials | Modified form of the R(-)-N-(4,4-di(3-methylthien-2-yl)but-3-enyl)-nipecotic acid hydrochloride |
US5753635A (en) | 1996-08-16 | 1998-05-19 | Berlex Laboratories, Inc. | Purine derivatives and their use as anti-coagulants |
AU720366B2 (en) | 1996-09-23 | 2000-06-01 | Eli Lilly And Company | Olanzapine dihydrate D |
AU4699697A (en) | 1996-10-28 | 1998-05-22 | Novo Nordisk A/S | A process for the preparation of (-)-3,4-trans-diarylchromans |
UA65549C2 (en) | 1996-11-05 | 2004-04-15 | Елі Ліллі Енд Компані | Use of glucagon-like peptides such as glp-1, glp-1 analog, or glp-1 derivative in methods and compositions for reducing body weight |
EP1529534B1 (en) | 1996-11-12 | 2007-07-11 | Novo Nordisk A/S | Use of GLP-1 peptides |
GB9623859D0 (en) | 1996-11-15 | 1997-01-08 | Chiroscience Ltd | Novel compounds |
KR20000069664A (en) | 1996-12-24 | 2000-11-25 | 아스트루 마이클 제이 | Stable liquid interferon formulations |
DE19705233A1 (en) | 1997-02-12 | 1998-08-13 | Froelich Juergen C | Preparation of stable, orally administered arginine solutions |
US6011049A (en) | 1997-02-19 | 2000-01-04 | Warner-Lambert Company | Combinations for diabetes |
BR9808581A (en) | 1997-03-13 | 2000-05-30 | Hexal Ag | Stabilization of acid-sensitive benzimidazoles with amino acid / cyclodextrin combinations |
US5972332A (en) | 1997-04-16 | 1999-10-26 | The Regents Of The University Of Michigan | Wound treatment with keratinocytes on a solid support enclosed in a porous material |
ZA984697B (en) | 1997-06-13 | 1999-12-01 | Lilly Co Eli | Stable insulin formulations. |
US6174548B1 (en) | 1998-08-28 | 2001-01-16 | Andrx Pharmaceuticals, Inc. | Omeprazole formulation |
IL136499A0 (en) * | 1997-12-05 | 2001-06-14 | Astrazeneca Uk Ltd Astrazeneca | Pyrrolo-, thieno-, furano- and pyrazolo-[3,4,d] pypyrrolo-, thieno-, furano- and pyrazolo-[3,4,d] pyridazinone compounds, process for their preparatioridaziones compounds, process for their preparation, pharmaceutical compositions containing them, a n, pharmaceutical compositions containing them, a process for prepating the pharmaceutical compositiprocess for preparing the pharmaceutical compositions, and use thereof ons, and use thereof |
ID21411A (en) | 1997-12-10 | 1999-06-10 | Takeda Chemical Industries Ltd | AGENTS TO TREAT GLUCOSE RESISTANCE THAT IS RISK OF HIGH DAMAGED |
JPH11193270A (en) | 1997-12-26 | 1999-07-21 | Koei Chem Co Ltd | Production of optically active 1-methyl-3-piperidinemethanol |
EP1300147A1 (en) * | 1998-01-05 | 2003-04-09 | Eisai Co. Ltd | Purine compounds and adenosine A2 receptor antagonist as preventive or therapeutic agent for diabetes mellitus |
US6803357B1 (en) | 1998-02-02 | 2004-10-12 | New England Medical Center Hospitals, Inc. | Method of regulating glucose metabolism, and reagents related thereto |
US20030013740A1 (en) | 1998-03-27 | 2003-01-16 | Martin P. Redmon | Stable dosage forms of fluoxetine and its enantiomers |
SK14742000A3 (en) | 1998-03-31 | 2001-03-12 | Nissan Chemical Industries, Ltd. | Pyridazinone hydrochloride compound and method for producing the same |
CA2268621A1 (en) | 1998-04-13 | 1999-10-13 | Takeda Chemical Industries, Ltd. | 2-pipirazinone-1-acetic acid derivative, production and use thereof |
US6207207B1 (en) | 1998-05-01 | 2001-03-27 | Mars, Incorporated | Coated confectionery having a crispy starch based center and method of preparation |
DE19823831A1 (en) * | 1998-05-28 | 1999-12-02 | Probiodrug Ges Fuer Arzneim | New pharmaceutical use of isoleucyl thiazolidide and its salts |
DE19828114A1 (en) | 1998-06-24 | 2000-01-27 | Probiodrug Ges Fuer Arzneim | Produgs of unstable inhibitors of dipeptidyl peptidase IV |
DE19828113A1 (en) | 1998-06-24 | 2000-01-05 | Probiodrug Ges Fuer Arzneim | Prodrugs of Dipeptidyl Peptidase IV Inhibitors |
CA2337015C (en) | 1998-07-15 | 2004-09-07 | Asahi Kasei Kogyo Kabushiki Kaisha | Excipient |
CO5150173A1 (en) | 1998-12-10 | 2002-04-29 | Novartis Ag | COMPOUNDS N- (REPLACED GLYCLE) -2-DIPEPTIDYL-IV PEPTIDASE INHIBITING CYANOPIRROLIDINS (DPP-IV) WHICH ARE EFFECTIVE IN THE TREATMENT OF CONDITIONS MEDIATED BY DPP-IV INHIBITION |
IT1312018B1 (en) | 1999-03-19 | 2002-04-04 | Fassi Aldo | IMPROVED PROCEDURE FOR THE PRODUCTION OF NON HYGROSCOPICIDAL SALTS OF L (-) - CARNITINE. |
AU4671100A (en) | 1999-04-30 | 2000-11-17 | City Of Hope | Method of inhibiting glycation product formation |
US20040152659A1 (en) | 1999-05-12 | 2004-08-05 | Fujisawa Pharmaceutical Co. Ltd. | Method for the treatment of parkinson's disease comprising administering an A1A2a receptor dual antagonist |
AU4431000A (en) | 1999-05-12 | 2000-12-05 | Fujisawa Pharmaceutical Co., Ltd. | Novel use |
AU5294100A (en) | 1999-05-27 | 2000-12-18 | University Of Virginia Patent Foundation | Method and compositions for treating the inflammatory response |
DE60034445T2 (en) | 1999-05-31 | 2008-01-03 | Mitsubishi Chemical Corp. | FREEZE-DRIED HGF PREPARATIONS |
ATE271922T1 (en) | 1999-06-01 | 2004-08-15 | Elan Pharma Int Ltd | SMALL MILL AND METHOD THEREOF |
US6545002B1 (en) | 1999-06-01 | 2003-04-08 | University Of Virginia Patent Foundation | Substituted 8-phenylxanthines useful as antagonists of A2B adenosine receptors |
PT1731511E (en) | 1999-06-21 | 2015-11-13 | Boehringer Ingelheim Pharma | Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof |
US6448323B1 (en) | 1999-07-09 | 2002-09-10 | Bpsi Holdings, Inc. | Film coatings and film coating compositions based on polyvinyl alcohol |
ES2166270B1 (en) | 1999-07-27 | 2003-04-01 | Almirall Prodesfarma Sa | DERIVATIVES OF 8-PHENYL-6,9-DIHIDRO- (1,2,4,) TRIAZOLO (3,4-I) PURIN-5-ONA. |
US6515117B2 (en) | 1999-10-12 | 2003-02-04 | Bristol-Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
US6586438B2 (en) | 1999-11-03 | 2003-07-01 | Bristol-Myers Squibb Co. | Antidiabetic formulation and method |
GB9928330D0 (en) | 1999-11-30 | 2000-01-26 | Ferring Bv | Novel antidiabetic agents |
KR20100130651A (en) | 1999-12-23 | 2010-12-13 | 노파르티스 아게 | Use of hypoglycemic agent for treating impaired glucose metabolism |
US20020048610A1 (en) | 2000-01-07 | 2002-04-25 | Cima Michael J. | High-throughput formation, identification, and analysis of diverse solid-forms |
US6362172B2 (en) | 2000-01-20 | 2002-03-26 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
DK1741445T3 (en) | 2000-01-21 | 2013-11-04 | Novartis Ag | Combinations comprising dipeptidyl peptidase IV inhibitors and antidiabetic agents |
JP4621326B2 (en) * | 2000-02-01 | 2011-01-26 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Teprenone stabilized composition |
IL145756A0 (en) * | 2000-02-05 | 2002-07-25 | Vertex Pharma | Pyrazole derivatives and pharmaceutical compositions containing the same |
CA2401356A1 (en) | 2000-02-24 | 2001-08-30 | Takeda Chemical Industries, Ltd. | Combination drug |
EP1132389A1 (en) | 2000-03-06 | 2001-09-12 | Vernalis Research Limited | New aza-indolyl derivatives for the treatment of obesity |
US6395767B2 (en) | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
GB0006133D0 (en) | 2000-03-14 | 2000-05-03 | Smithkline Beecham Plc | Novel pharmaceutical |
JP2001278812A (en) * | 2000-03-27 | 2001-10-10 | Kyoto Pharmaceutical Industries Ltd | Disintegrant for tablet and tablet using the same |
US6399101B1 (en) | 2000-03-30 | 2002-06-04 | Mova Pharmaceutical Corp. | Stable thyroid hormone preparations and method of making same |
MXPA02009485A (en) | 2000-03-31 | 2003-03-10 | Kirin Brewery | Powdery preparation for transmucosal administration containing a polymeric form of drug and exhibiting improved storage stability. |
KR20080067009A (en) | 2000-03-31 | 2008-07-17 | 프로시디온 리미티드 | A pharmaceutical composition comprising dipeptidyl peptidase iv enzyme activity inhibitor |
JP2001292388A (en) | 2000-04-05 | 2001-10-19 | Sharp Corp | Reproducing device |
GB0008694D0 (en) | 2000-04-07 | 2000-05-31 | Novartis Ag | Organic compounds |
US6962998B2 (en) | 2000-06-14 | 2005-11-08 | Toray Industries, Inc. | Processes for producing racemic piperidine derivative and for producing optically active piperidine derivative |
GB0014969D0 (en) | 2000-06-19 | 2000-08-09 | Smithkline Beecham Plc | Novel method of treatment |
US7078397B2 (en) | 2000-06-19 | 2006-07-18 | Smithkline Beecham Corporation | Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus |
US6689353B1 (en) | 2000-06-28 | 2004-02-10 | Bayer Pharmaceuticals Corporation | Stabilized interleukin 2 |
HUP0301622A3 (en) * | 2000-07-04 | 2006-05-29 | Novo Nordisk As | Purine derivatives inhibiting the enzyme dipeptidyl petidase iv (dpp-iv) and pharmaceutical compositions containing them |
ES2334858T3 (en) * | 2000-08-10 | 2010-03-16 | Mitsubishi Tanabe Pharma Corporation | DERIVATIVES OF PROLINA AND USE OF THE SAME AS PHARMACOS. |
US6821978B2 (en) | 2000-09-19 | 2004-11-23 | Schering Corporation | Xanthine phosphodiesterase V inhibitors |
WO2004081006A1 (en) | 2003-03-12 | 2004-09-23 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Weak base salts |
US20060034922A1 (en) | 2000-11-03 | 2006-02-16 | Andrx Labs, Llc | Controlled release metformin compositions |
US6722883B2 (en) | 2000-11-13 | 2004-04-20 | G & H Technologies Llc | Protective coating for abrasive dental tools and burs |
US6821261B2 (en) | 2000-12-12 | 2004-11-23 | Dj Orthopedics, Llc | Orthopedic brace having length-adjustable supports |
EP1354882A1 (en) | 2000-12-27 | 2003-10-22 | Kyowa Hakko Kogyo Co., Ltd. | Dipeptidyl peptidase iv inhibitor |
FR2818906B1 (en) | 2000-12-29 | 2004-04-02 | Dospharma | DRUG ASSOCIATION OF A BIGUANINE AND A CARRIER, FOR EXAMPLE OF METFORMIN AND ARGININE |
FR2819254B1 (en) | 2001-01-08 | 2003-04-18 | Fournier Lab Sa | NOVEL N- (PHENYLSULFONYL) GLYCINE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THEIR USE FOR OBTAINING PHARMACEUTICAL COMPOSITIONS |
DE10109021A1 (en) | 2001-02-24 | 2002-09-05 | Boehringer Ingelheim Pharma | New 8-substituted-xanthine derivatives, useful e.g. for treating diabetes and arthritis, act by inhibiting dipeptidylpeptidase-IV |
DE10117803A1 (en) | 2001-04-10 | 2002-10-24 | Boehringer Ingelheim Pharma | New 8-substituted-xanthine derivatives, useful e.g. for treating diabetes and arthritis, act by inhibiting dipeptidylpeptidase-IV |
SK10802003A3 (en) | 2001-02-02 | 2004-05-04 | Takeda Chemical Industries, Ltd. | Fused heterocyclic compounds |
US6610326B2 (en) | 2001-02-16 | 2003-08-26 | Andrx Corporation | Divalproex sodium tablets |
WO2002066015A1 (en) | 2001-02-16 | 2002-08-29 | Bristol-Myers Squibb Pharma Company | Use of polyalkylamine polymers in controlled release devices |
EP1953162B9 (en) * | 2001-02-24 | 2012-10-31 | Boehringer Ingelheim Pharma GmbH & Co. KG | Xanthin derivatives, their production and utilisation as medicine |
US6936590B2 (en) | 2001-03-13 | 2005-08-30 | Bristol Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
US6693094B2 (en) | 2001-03-22 | 2004-02-17 | Chrono Rx Llc | Biguanide and sulfonylurea formulations for the prevention and treatment of insulin resistance and type 2 diabetes mellitus |
JP2002348279A (en) | 2001-05-25 | 2002-12-04 | Nippon Kayaku Co Ltd | Production method for optically active pyridylketone derivatives and optically active pyridylketone derivatives |
DE10130371A1 (en) | 2001-06-23 | 2003-01-02 | Boehringer Ingelheim Pharma | New drug compositions based on anticholinergics, corticosteroids and betamimetics |
GB0115517D0 (en) | 2001-06-25 | 2001-08-15 | Ferring Bv | Novel antidiabetic agents |
WO2003002531A2 (en) | 2001-06-27 | 2003-01-09 | Smithkline Beecham Corporation | Fluoropyrrolidines as dipeptidyl peptidase inhibitors |
JP4357293B2 (en) | 2001-06-27 | 2009-11-04 | スミスクライン ビーチャム コーポレーション | Fluoropyrrolidines as dipeptidyl peptidase inhibitors |
US6869947B2 (en) * | 2001-07-03 | 2005-03-22 | Novo Nordisk A/S | Heterocyclic compounds that are inhibitors of the enzyme DPP-IV |
ATE388951T1 (en) | 2001-07-03 | 2008-03-15 | Novo Nordisk As | DPP-IV INHIBITING PURINE DERIVATIVES FOR THE TREATMENT OF DIABETES |
UA74912C2 (en) | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
MXPA04000224A (en) | 2001-07-10 | 2005-07-25 | 4Sc Ag | Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents. |
US7085258B2 (en) * | 2001-07-19 | 2006-08-01 | International Business Machines Corporation | Instant messaging with voice conversation feature |
US7638522B2 (en) | 2001-08-13 | 2009-12-29 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile |
AR035119A1 (en) | 2001-08-16 | 2004-04-14 | Lilly Co Eli | ANTI-HTNFSF13B HUMAN ANTI-BODIES |
CA2460512A1 (en) | 2001-09-14 | 2003-03-27 | Mitsubishi Pharma Corporation | Thiazolidine derivatives and medicinal use thereof |
JP2005509603A (en) | 2001-09-19 | 2005-04-14 | ノボ ノルディスク アクティーゼルスカブ | Heterocyclic compounds that are inhibitors of the DPP-IV enzyme |
CN1568166A (en) | 2001-10-15 | 2005-01-19 | 荷姆泰克股份有限公司 | Coating of stents for preventing restenosis |
DE10151296A1 (en) | 2001-10-17 | 2003-04-30 | Boehringer Ingelheim Pharma | Keratinocytes useful as a biologically active substance in the treatment of wounds |
US6723340B2 (en) | 2001-10-25 | 2004-04-20 | Depomed, Inc. | Optimal polymer mixtures for gastric retentive tablets |
US6861440B2 (en) | 2001-10-26 | 2005-03-01 | Hoffmann-La Roche Inc. | DPP IV inhibitors |
US20030083354A1 (en) | 2001-10-26 | 2003-05-01 | Pediamed Pharmaceuticals, Inc. | Phenylephrine tannate and pyrilamine tannate salts in pharmaceutical compositions |
CA2363053C (en) | 2001-11-09 | 2011-01-25 | Bernard Charles Sherman | Clopidogrel bisulfate tablet formulation |
EP1457487A4 (en) | 2001-12-21 | 2005-06-22 | Toray Finechemicals Co Ltd | Process for production of optically active cis-piperidine derivatives |
US6727261B2 (en) | 2001-12-27 | 2004-04-27 | Hoffman-La Roche Inc. | Pyrido[2,1-A]Isoquinoline derivatives |
WO2003057245A1 (en) | 2001-12-28 | 2003-07-17 | Nrl Pharma, Inc. | Compositions for improving lipid metabolism |
US20070197552A1 (en) | 2002-01-11 | 2007-08-23 | Novo Nordisk A/S | Method and composition for treatment of diabetes, hypertension, chronic heart failure and fluid retentive states |
WO2003057200A2 (en) | 2002-01-11 | 2003-07-17 | Novo Nordisk A/S | Compositions comprising inhibitors of dpp-iv and nep enzymes for the treatment of diabetes |
EP2260833B1 (en) | 2002-01-16 | 2012-11-21 | Boehringer Ingelheim Pharma GmbH & Co. KG | Bilayer pharmaceutical tablet comprising telmisartan and a diuretic |
EP1477182A4 (en) | 2002-01-21 | 2009-05-27 | Nrl Pharma Inc | Novel analgesics |
EP1333033A1 (en) | 2002-01-30 | 2003-08-06 | Boehringer Ingelheim Pharma GmbH & Co.KG | FAP-activated anti-tumor compounds |
RU2004123621A (en) * | 2002-02-01 | 2005-04-10 | Пфайзер Продактс Инк. (Us) | MEDICINAL FORMS WITH IMMEDIATE RELEASE CONTAINING SOLID DISPERSIONS OF MEDICINES |
US7610153B2 (en) | 2002-02-13 | 2009-10-27 | Virginia Commonwealth University | Multi-drug titration and evaluation |
EP1476139B1 (en) | 2002-02-21 | 2017-05-17 | Valeant Pharmaceuticals Luxembourg S.à.r.l. | Controlled release dosage forms |
EP1338595B1 (en) | 2002-02-25 | 2006-05-03 | Eisai Co., Ltd. | Xanthine derivatives as DPP-IV inhibitors |
HUP0200849A2 (en) | 2002-03-06 | 2004-08-30 | Sanofi-Synthelabo | N-aminoacetyl-pyrrolidine-2-carbonitrile derivatives, pharmaceutical compositions containing them and process for producing them |
JP4298212B2 (en) | 2002-03-29 | 2009-07-15 | 大日本印刷株式会社 | Method for producing high melting point type epinastine hydrochloride |
JP2003300977A (en) | 2002-04-10 | 2003-10-21 | Sumitomo Pharmaceut Co Ltd | Xanthine derivative |
US20050113577A1 (en) | 2002-04-16 | 2005-05-26 | Karki Shyam B. | Solid forms of slats with tyrosine kinase activity |
CA2484306A1 (en) | 2002-04-26 | 2003-11-06 | Katsumi Maezono | Prophylactic and therapeutic agent of diabetes mellitus |
AU2003231252A1 (en) | 2002-05-09 | 2003-11-11 | Enos Pharmaceuticals, Inc. | Methods and compositions for the treatment and prevention of intermittent claudication or alzheimer's disease |
GB0212412D0 (en) | 2002-05-29 | 2002-07-10 | Novartis Ag | Combination of organic compounds |
CN101538224A (en) | 2002-05-31 | 2009-09-23 | 先灵公司 | Process for preparing xanthine phosphodiesterase V inhibitors and precursers thereof |
MXPA04012226A (en) * | 2002-06-06 | 2005-04-08 | Eisai Co Ltd | Novel fused imidazole derivative. |
ES2199061B1 (en) * | 2002-06-10 | 2005-02-16 | Laboratorios Vita, S.A. | TROUBLE-BASED TABLETS AND PROCEDURE FOR OBTAINING. |
FR2840897B1 (en) | 2002-06-14 | 2004-09-10 | Fournier Lab Sa | NOVEL ARYLSULFONAMIDE DERIVATIVES AND THEIR USE IN THERAPEUTICS |
US20040002615A1 (en) | 2002-06-28 | 2004-01-01 | Allen David Robert | Preparation of chiral amino-nitriles |
US7065367B2 (en) * | 2002-07-11 | 2006-06-20 | Oliver Michaelis | Interface selection in a wireless communication network |
US20040023981A1 (en) | 2002-07-24 | 2004-02-05 | Yu Ren | Salt forms with tyrosine kinase activity |
TW200409746A (en) | 2002-07-26 | 2004-06-16 | Theravance Inc | Crystalline β2 adrenergic receptor agonist |
TW200404796A (en) | 2002-08-19 | 2004-04-01 | Ono Pharmaceutical Co | Nitrogen-containing compound |
US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
BR122012026540B8 (en) * | 2002-08-21 | 2021-05-25 | Boehringer Ingelheim Pharma | 8-[3-amino-piperidin-1-yl]-xanthines, their pharmaceutically acceptable salts, their use and their preparation process, as well as medicine and their preparation process |
DE10238243A1 (en) | 2002-08-21 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New 8-(3-amino-piperidin-1-yl)-xanthine derivatives are dipeptidylpeptidase-IV inhibitors useful for, e.g. treating diabetes mellitus, arthritis or obesity |
US7569574B2 (en) * | 2002-08-22 | 2009-08-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Purine derivatives, the preparation thereof and their use as pharmaceutical compositions |
US7495005B2 (en) | 2002-08-22 | 2009-02-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, their preparation and their use in pharmaceutical compositions |
DE10238477A1 (en) | 2002-08-22 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New purine derivatives, their production and their use as medicines |
DE10238470A1 (en) | 2002-08-22 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New xanthine derivatives, their production and their use as medicines |
DE10238723A1 (en) | 2002-08-23 | 2004-03-11 | Bayer Ag | Phenyl substituted pyrazolyprimidines |
DE10238724A1 (en) | 2002-08-23 | 2004-03-04 | Bayer Ag | New 6-alkyl-1,5-dihydro-4H-pyrazolo-(3,4-d)-pyrimidin-4-ones useful as selective phosphodiesterase 9A inhibitors for improving attention, concentration, learning and/or memory performance |
JP2004123738A (en) * | 2002-09-11 | 2004-04-22 | Takeda Chem Ind Ltd | Sustained-release preparation |
US20060039974A1 (en) * | 2002-09-11 | 2006-02-23 | Takeda Pharmaceutical Company Limited | Sustained release preparation |
CA2498931A1 (en) * | 2002-09-16 | 2004-03-25 | Wyeth | Delayed release formulations for oral administration of a polypeptide therapeutic agent and methods of using same |
US20060094722A1 (en) * | 2002-09-26 | 2006-05-04 | Eisai Co., Ltd. | Combination drug |
AU2003267732A1 (en) * | 2002-10-08 | 2004-05-04 | Ranbaxy Laboratories Limited | Gabapentin tablets and methods for their preparation |
AU2003269850A1 (en) | 2002-10-08 | 2004-05-04 | Novo Nordisk A/S | Hemisuccinate salts of heterocyclic dpp-iv inhibitors |
US20040122048A1 (en) | 2002-10-11 | 2004-06-24 | Wyeth Holdings Corporation | Stabilized pharmaceutical composition containing basic excipients |
US6861526B2 (en) | 2002-10-16 | 2005-03-01 | Pfizer Inc. | Process for the preparation of (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine |
PT1556362E (en) | 2002-10-18 | 2008-06-16 | Merck & Co Inc | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
JP2004161749A (en) | 2002-10-24 | 2004-06-10 | Toray Fine Chemicals Co Ltd | Method for producing optically active, nitrogen-containing compound |
AU2003280680A1 (en) | 2002-11-01 | 2004-06-18 | Sumitomo Pharmaceuticals Co., Ltd. | Xanthine compound |
BR0315796A (en) | 2002-11-07 | 2005-09-13 | Merck & Co Inc | Compound, Pharmaceutical Composition, and, Methods for Treating Diabetes, Treating Hyperglycemia, and Treating Obesity in a Mammal |
US7482337B2 (en) * | 2002-11-08 | 2009-01-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions |
DE10251927A1 (en) | 2002-11-08 | 2004-05-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New 1,7,8-trisubstituted xanthine derivatives, are dipeptidylpeptidase-IV inhibitors useful e.g. for treating diabetes mellitus type I or II, arthritis or obesity |
DE10254304A1 (en) * | 2002-11-21 | 2004-06-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New xanthine derivatives, their production and their use as medicines |
UY28103A1 (en) | 2002-12-03 | 2004-06-30 | Boehringer Ingelheim Pharma | NEW IMIDAZO-PIRIDINONAS REPLACED, ITS PREPARATION AND ITS EMPLOYMENT AS MEDICATIONS |
US7109192B2 (en) * | 2002-12-03 | 2006-09-19 | Boehringer Ingelheim Pharma Gmbh & Co Kg | Substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions |
JP2006512334A (en) | 2002-12-10 | 2006-04-13 | ノバルティス アクチエンゲゼルシャフト | Combination of DPP-IV inhibitor and PPAR-alpha compound |
DE10351663A1 (en) | 2002-12-20 | 2004-07-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Stable, accurately dosable inhalable powder medicament for treating asthma or chronic obstructive pulmonary disease, containing tiotropium, specific form of salmeterol xinafoate and auxiliary |
US20040152720A1 (en) | 2002-12-20 | 2004-08-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Powdered medicaments containing a tiotropium salt and salmeterol xinafoate |
SI1599222T1 (en) | 2003-01-08 | 2009-08-31 | Novartis Vaccines & Diagnostic | Stabilized aqueous compositions comprising tissue factor pathway inhibitor (tfpi) or tissue factor pathway inhibitor variant |
PL377847A1 (en) | 2003-01-14 | 2006-02-20 | Arena Pharmaceuticals Inc. | 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prpphylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia |
DE10335027A1 (en) | 2003-07-31 | 2005-02-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Use of telmisartan and simvastatin for treatment or prophylaxis of cardiovascular, cardiopulmonary and renal diseases e.g. hypertension combined with hyperlipidemia or atherosclerosis |
PE20040950A1 (en) | 2003-02-14 | 2005-01-01 | Theravance Inc | BIPHENYL DERIVATIVES AS AGONISTS OF ß2-ADRENERGIC RECEPTORS AND AS ANTAGONISTS OF MUSCARINAL RECEPTORS |
JP2004250336A (en) * | 2003-02-18 | 2004-09-09 | Kao Corp | Method for producing coated tablet and sugar-coated tablet |
US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
US7442387B2 (en) | 2003-03-06 | 2008-10-28 | Astellas Pharma Inc. | Pharmaceutical composition for controlled release of active substances and manufacturing method thereof |
US20060159746A1 (en) | 2003-03-18 | 2006-07-20 | Troup John P | Compositions comprising fatty acids and amino acids |
DK2368554T3 (en) | 2003-04-08 | 2015-01-26 | Progenics Pharm Inc | A pharmaceutical composition comprising methylnaltrexone |
US20040220186A1 (en) | 2003-04-30 | 2004-11-04 | Pfizer Inc. | PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease |
JPWO2004096806A1 (en) | 2003-04-30 | 2006-07-13 | 大日本住友製薬株式会社 | Condensed imidazole derivatives |
TW200510277A (en) | 2003-05-27 | 2005-03-16 | Theravance Inc | Crystalline form of β2-adrenergic receptor agonist |
FR2855521B1 (en) | 2003-05-28 | 2005-08-05 | Flamel Tech Sa | POLYAMINOACIDES FUNCTIONALIZED BY AT LEAST ONE YDROPHOBIC GROUP AND THEIR PARTICULARLY THERAPEUTIC APPLICATIONS. |
AU2003902828A0 (en) | 2003-06-05 | 2003-06-26 | Fujisawa Pharmaceutical Co., Ltd. | Dpp-iv inhibitor |
US7566707B2 (en) * | 2003-06-18 | 2009-07-28 | Boehringer Ingelheim International Gmbh | Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions |
DE10327439A1 (en) | 2003-06-18 | 2005-01-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel imidazopyridazinone and imidazopyridone derivatives, their production and their use as pharmaceuticals |
SI1638970T1 (en) | 2003-06-20 | 2011-03-31 | Hoffmann La Roche | Pyrid (2, 1-a) - isoquinoline derivatives as dpp-iv inhibitors |
MXPA05013734A (en) | 2003-06-20 | 2006-03-08 | Hoffmann La Roche | Hexahydropyridoisoqinolines as dpp-iv inhibitors. |
JO2625B1 (en) * | 2003-06-24 | 2011-11-01 | ميرك شارب اند دوم كوربوريشن | Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor |
US7364755B2 (en) | 2003-07-07 | 2008-04-29 | Synthon Ip Inc. | Modified calcium phosphate excipient |
AR045047A1 (en) | 2003-07-11 | 2005-10-12 | Arena Pharm Inc | ARILO AND HETEROARILO DERIVATIVES TRISUSTITUIDOS AS MODULATORS OF METABOLISM AND PROFILAXIS AND TREATMENT OF DISORDERS RELATED TO THEMSELVES |
EA010023B1 (en) | 2003-07-14 | 2008-06-30 | Арена Фармасьютикалз, Инк. | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
US20050027012A1 (en) | 2003-07-16 | 2005-02-03 | Boehringer Ingelheim International Gmbh | Tablets containing ambroxol |
ATE457166T1 (en) | 2003-07-24 | 2010-02-15 | Wockhardt Ltd | ORAL COMPOSITIONS FOR TREATING DIABETES |
JP2007501189A (en) * | 2003-08-01 | 2007-01-25 | ジェネラブス テクノロジーズ,インコーポレイテッド | Bicyclic imidazole derivatives for Flaviviridae |
US6995183B2 (en) | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
EP1656158B1 (en) | 2003-08-14 | 2016-03-09 | Novo Nordisk Health Care AG | Liquid, aqueous pharmaceutical composition of factor vii polypeptides |
CN101856348A (en) * | 2003-08-29 | 2010-10-13 | 斯隆-凯特林癌症研究所 | The therapeutic alliance method for cancer |
US7790734B2 (en) | 2003-09-08 | 2010-09-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
WO2005032590A1 (en) | 2003-10-03 | 2005-04-14 | Takeda Pharmaceutical Company Limited | Remedy for diabetes |
US7107714B2 (en) | 2003-11-10 | 2006-09-19 | Marketing Displays, Inc. | Portable snap-fit sign stand |
JP2007511487A (en) | 2003-11-17 | 2007-05-10 | ノバルティス アクチエンゲゼルシャフト | Use of dipeptidyl peptidase IV inhibitors |
DE10355304A1 (en) | 2003-11-27 | 2005-06-23 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel 8- (piperazin-1-yl) and 8 - ([1,4] diazepan-1-yl) xanthines, their preparation and their use as pharmaceuticals |
WO2005053695A1 (en) * | 2003-12-04 | 2005-06-16 | Eisai Co., Ltd. | Preventive or therapeutic agent for multiple sclerosis |
DE10359098A1 (en) | 2003-12-17 | 2005-07-28 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel 2- (piperazin-1-yl) and 2 - ([1,4] diazepan-1-yl) imidazo [4,5-d] pyridazin-4-ones, their preparation and their use as pharmaceuticals |
US7217711B2 (en) * | 2003-12-17 | 2007-05-15 | Boehringer Ingelheim International Gmbh | Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions |
DE602004031776D1 (en) * | 2003-12-18 | 2011-04-21 | Tibotec Pharm Ltd | PIPERIDINAMINO BENZIMIDAZOLE DERIVATIVES AL RESPIRATORY SYNCYTIALVIRUS REPLICATION INHIBITORS |
DE10360835A1 (en) | 2003-12-23 | 2005-07-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New bicyclic imidazole derivatives are dipeptidylpeptidase-IV inhibitors useful to treat e.g. arthritis, obesity, allograft transplantation and calcitonin-induced osteoporosis |
JP4958560B2 (en) | 2003-12-24 | 2012-06-20 | プロシディオン・リミテッド | Heterocyclic derivatives as GPCR receptor agonists |
AU2005205933B2 (en) | 2004-01-21 | 2010-02-18 | Elanco Animal Health Ireland Limited | Mitratapide oral solution |
SE0400234D0 (en) | 2004-02-06 | 2004-02-06 | Active Biotech Ab | New compounds, methods for their preparation and use thereof |
US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
CN102199151A (en) * | 2004-02-18 | 2011-09-28 | 贝林格尔.英格海姆国际有限公司 | 8-[3-amino-piperidin-1-yl]-xanthine, the production thereof and the use |
DE102004019540A1 (en) | 2004-04-22 | 2005-11-10 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Composition, useful for treatment of e.g. inflammatory and obstructive respiratory complaint, sinus rhythm in heart in atrioventricular block and circulatory shock, comprises 6-hydroxy-4H-benzo1,4oxazin-3-one derivatives and other actives |
DE102004009039A1 (en) * | 2004-02-23 | 2005-09-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8- [3-Amino-piperidin-1-yl] xanthines, their preparation and use as pharmaceuticals |
EP1593671A1 (en) | 2004-03-05 | 2005-11-09 | Graffinity Pharmaceuticals AG | DPP-IV inhibitors |
US7393847B2 (en) * | 2004-03-13 | 2008-07-01 | Boehringer Ingleheim International Gmbh | Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions |
CN102134229B (en) | 2004-03-15 | 2020-08-04 | 武田药品工业株式会社 | Dipeptidyl peptidase inhibitors |
CN103435581B (en) | 2004-03-16 | 2015-08-19 | 贝林格尔.英格海姆国际有限公司 | The phenyl derivatives that glucopyranosyl replaces, medicine, its purposes and manufacture method thereof containing this compound |
EP1577306A1 (en) | 2004-03-17 | 2005-09-21 | Boehringer Ingelheim Pharma GmbH & Co.KG | novel benzoxazinone derivatives as slow-acting betamimetics and use thereof in treatment of respiratory tract diseases |
US7179809B2 (en) | 2004-04-10 | 2007-02-20 | Boehringer Ingelheim International Gmbh | 2-Amino-imidazo[4,5-d]pyridazin-4-ones, their preparation and their use as pharmaceutical compositions |
WO2005097798A1 (en) | 2004-04-10 | 2005-10-20 | Boehringer Ingelheim International Gmbh | Novel 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones, production and use thereof as medicaments |
US20050239778A1 (en) | 2004-04-22 | 2005-10-27 | Boehringer Ingelheim International Gmbh | Novel medicament combinations for the treatment of respiratory diseases |
US20050244502A1 (en) | 2004-04-28 | 2005-11-03 | Mathias Neil R | Composition for enhancing absorption of a drug and method |
CA2565250C (en) | 2004-05-03 | 2013-11-12 | Omega Bio-Pharma (I.P.3) Limited | Cysteamines for treating complications of hypercholesterolemia and diabetes |
US7439370B2 (en) * | 2004-05-10 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides |
KR100869616B1 (en) | 2004-05-12 | 2008-11-21 | 화이자 프로덕츠 인코포레이티드 | Proline derivatives and their use as dipeptidyl peptidase iv inhibitors |
DE102004024454A1 (en) | 2004-05-14 | 2005-12-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel enantiomerically pure beta agonists, process for their preparation and their use as pharmaceuticals |
PE20060315A1 (en) | 2004-05-24 | 2006-05-15 | Irm Llc | THIAZOLE COMPOUNDS AS PPAR MODULATORS |
TWI415635B (en) * | 2004-05-28 | 2013-11-21 | 必治妥施貴寶公司 | Coated tablet formulation and method |
WO2005117948A1 (en) | 2004-06-01 | 2005-12-15 | Ares Trading S.A. | Method of stabilizing proteins |
WO2005117861A1 (en) | 2004-06-04 | 2005-12-15 | Novartis Ag | Use of organic compounds |
WO2005120576A2 (en) | 2004-06-09 | 2005-12-22 | Yasoo Health | Composition and method for improving pancreatic islet cell survival |
DE102004030502A1 (en) | 2004-06-24 | 2006-01-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel imidazoles and triazoles, their preparation and use as medicines |
CA2511269A1 (en) | 2004-07-07 | 2006-01-07 | F. Hoffmann-La Roche Ag | Multimarker panel based on p1gf for diabetes type 1 and 2 |
JP2008506651A (en) | 2004-07-14 | 2008-03-06 | ノバルティス アクチエンゲゼルシャフト | Combination of a DPP-IV inhibitor and a compound that modulates 5-HT3 and / or 5-HT4 receptor |
JP2006045156A (en) | 2004-08-06 | 2006-02-16 | Sumitomo Pharmaceut Co Ltd | Condensed pyrazole derivative |
TW200613275A (en) | 2004-08-24 | 2006-05-01 | Recordati Ireland Ltd | Lercanidipine salts |
JP4854511B2 (en) | 2004-08-26 | 2012-01-18 | 武田薬品工業株式会社 | Diabetes treatment |
DE102004043944A1 (en) | 2004-09-11 | 2006-03-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Novel 8- (3-amino-piperidin-1-yl) -7- (but-2-ynyl) -xanthines, their preparation and their use as pharmaceuticals |
DE102004044221A1 (en) | 2004-09-14 | 2006-03-16 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New 3-methyl-7-butynyl xanthines, their preparation and their use as pharmaceuticals |
CN1759834B (en) | 2004-09-17 | 2010-06-23 | 中国医学科学院医药生物技术研究所 | Application of berberine or associated with Simvastatin in preparing product for preventing or curing disease or symptom related to blood fat |
AU2005289881A1 (en) | 2004-09-23 | 2006-04-06 | Amgen Inc. | Substituted sulfonamidopropionamides and methods of use |
KR20070099527A (en) | 2004-10-08 | 2007-10-09 | 노파르티스 아게 | Combination of organic compounds |
EP1799639B1 (en) | 2004-10-12 | 2013-09-04 | Glenmark Pharmaceuticals S.A. | Novel dipeptidyl peptidase iv inhibitors, pharmaceutical compositions containing them, and process for their preparation |
KR20070068407A (en) | 2004-10-25 | 2007-06-29 | 노파르티스 아게 | Combination of dpp-iv inhibitor, ppar antidiabetic and metformin |
DE102004054054A1 (en) * | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Process for preparing chiral 8- (3-amino-piperidin-1-yl) -xanthines |
DE102005013967A1 (en) | 2004-11-05 | 2006-10-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | New imidazole or pyrimidine derivatives are bradykinin B1 antagonists used for treating e.g. pain, stroke, peptic ulcers and other inflammatory disorders |
JP2006137678A (en) | 2004-11-10 | 2006-06-01 | Shionogi & Co Ltd | Interleukin-2 composition |
BRPI0518651A2 (en) | 2004-12-24 | 2008-12-02 | Dainippon Sumitomo Pharma | compound, a prodrug thereof, or a pharmaceutically acceptable compound or prodrug salt, pharmaceutical composition, dipeptidyl peptidase iv inhibitor, use of a compound, a prodrug thereof or a compound or prodrug salt pharmaceutically acceptable method of treating diabetes |
KR100760430B1 (en) | 2004-12-31 | 2007-10-04 | 한미약품 주식회사 | Controlled release complex formulation for oral administration of medicine for diabetes and method for the preparation thereof |
MY148521A (en) | 2005-01-10 | 2013-04-30 | Arena Pharm Inc | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto |
DOP2006000008A (en) | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | COMBINED THERAPY FOR THE TREATMENT OF DIABETES AND RELATED AFFECTIONS AND FOR THE TREATMENT OF AFFECTIONS THAT IMPROVE THROUGH AN INCREASE IN THE BLOOD CONCENTRATION OF GLP-1 |
GT200600008A (en) | 2005-01-18 | 2006-08-09 | FORMULATION OF DIRECT COMPRESSION AND PROCESS | |
JP2008536881A (en) | 2005-04-21 | 2008-09-11 | ガストロテック・ファルマ・アクティーゼルスカブ | Pharmaceutical formulation of GLP-1 molecule and antiemetic |
ZA200708179B (en) | 2005-04-22 | 2009-12-30 | Alantos Pharmaceuticals Holding Inc | Dipeptidyl peptidase-IV inhibitors |
UA91546C2 (en) | 2005-05-03 | 2010-08-10 | Бьорінгер Інгельхайм Інтернаціональ Гмбх | Crystalline form of 1-chloro-4-(я-d-glucopyranos-1-yl)-2-[4-((s)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments |
EP1883631A1 (en) | 2005-05-25 | 2008-02-06 | Wyeth | Methods of synthesizing substituted 3-cyanoquinolines and intermediates thereof |
US8754032B2 (en) | 2005-06-03 | 2014-06-17 | Mitsubishi Tanabe Pharma Corporation | Concomitant pharmaceutical agents and use thereof |
GT200600218A (en) | 2005-06-10 | 2007-03-28 | FORMULATION AND PROCESS OF DIRECT COMPRESSION | |
CA2612475C (en) | 2005-06-20 | 2015-07-28 | Decode Genetics Ehf. | Genetic variants in the tcf7l2 gene as diagnostic markers for risk of type 2 diabetes mellitus |
ATE483732T1 (en) | 2005-07-08 | 2010-10-15 | Pfizer Ltd | MADCAM ANTIBODIES |
UY29694A1 (en) | 2005-07-28 | 2007-02-28 | Boehringer Ingelheim Int | METHODS TO PREVENT AND TREAT METABOLIC AND NEW DISORDERS DERIVED FROM PIRAZOL-O-GLUCOSIDO |
DE102005035891A1 (en) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8- (3-amino-piperidin-1-yl) -xanthines, their preparation and their use as pharmaceuticals |
KR20080030652A (en) * | 2005-08-11 | 2008-04-04 | 에프. 호프만-라 로슈 아게 | Pharmaceutical composition comprising a dpp-iv inhibitor |
EP1760076A1 (en) | 2005-09-02 | 2007-03-07 | Ferring B.V. | FAP Inhibitors |
PL1942898T5 (en) | 2005-09-14 | 2014-10-31 | Takeda Pharmaceuticals Co | Dipeptidyl peptidase inhibitors for treating diabetes |
KR101352588B1 (en) | 2005-09-14 | 2014-01-17 | 다케다 야쿠힌 고교 가부시키가이샤 | Dipeptidyl peptidase inhibitors for treating diabetis |
NZ565898A (en) | 2005-09-16 | 2010-07-30 | Arena Pharm Inc | Modulators of metabolism and the treatment of disorders related thereto |
RU2440143C2 (en) | 2005-09-20 | 2012-01-20 | Новартис Аг | Application of dpp-iv inhibitor for reduction of glycemia acute exacerbation |
WO2007038979A1 (en) | 2005-09-22 | 2007-04-12 | Swissco Development Ag | Effervescent metformin composition and tablets and granules made therefrom |
JOP20180109A1 (en) | 2005-09-29 | 2019-01-30 | Novartis Ag | New Formulation |
RU2008116578A (en) | 2005-09-30 | 2009-11-10 | Новартис АГ (CH) | APPLICATION OF DPP-IV INHIBITORS FOR TREATMENT OF AUTOIMMUNE DISEASES AND TRANSPLANT rejection |
JP2009513633A (en) | 2005-10-25 | 2009-04-02 | メルク エンド カムパニー インコーポレーテッド | Combination of dipeptidyl peptidase-4 inhibitor and antihypertensive agent for the treatment of diabetes and hypertension |
KR100945632B1 (en) | 2005-11-04 | 2010-03-04 | 엘에스전선 주식회사 | Synthesis of MDH-polymer hybrid paticles |
CA2633167A1 (en) | 2005-12-16 | 2007-07-12 | Merck & Co., Inc. | Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin |
GB0526291D0 (en) | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
EP1966215A1 (en) | 2005-12-23 | 2008-09-10 | Novartis AG | Condensed heterocyclic compounds useful as dpp-iv inhibitors |
JP2009522374A (en) | 2006-01-06 | 2009-06-11 | ノバルティス アクチエンゲゼルシャフト | Use of vildagliptin for the treatment of diabetes |
TW200801029A (en) | 2006-02-15 | 2008-01-01 | Boehringer Ingelheim Int | Glucopyranosyl-substituted benzonitrile derivatives, pharmaceutical compositions containing such compounds, their use and process for their manufacture |
WO2007099345A1 (en) | 2006-03-02 | 2007-09-07 | Betagenon Ab | Medical use of bmp-2 and/ or bmp-4 |
PE20071221A1 (en) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | GPR119 RECEPTOR AGONISTS IN METHODS TO INCREASE BONE MASS AND TO TREAT OSTEOPOROSIS AND OTHER CONDITIONS CHARACTERIZED BY LOW BONE MASS, AND COMBINED THERAPY RELATED TO THESE AGONISTS |
US8455435B2 (en) | 2006-04-19 | 2013-06-04 | Ludwig-Maximilians-Universitat Munchen | Remedies for ischemia |
EA030606B1 (en) | 2006-05-04 | 2018-08-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Methods of preparing a medicament comprising polymorphs |
PE20110235A1 (en) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | PHARMACEUTICAL COMBINATIONS INCLUDING LINAGLIPTIN AND METMORPHINE |
EP1852108A1 (en) * | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
KR20070111099A (en) | 2006-05-16 | 2007-11-21 | 영진약품공업주식회사 | Novel crystalline form of sitagliptin hydrochloride |
CN101442994B (en) | 2006-05-16 | 2013-03-06 | 吉里德科学公司 | Methods and compositions for treating hematological malignancies |
US20080064717A1 (en) | 2006-05-19 | 2008-03-13 | Rajesh Iyengar | Inhibitors of diacylglycerol O-acyltransferase type 1 enzyme |
KR100858848B1 (en) | 2006-05-23 | 2008-09-17 | 한올제약주식회사 | Pharmaceutical compositions and formulations of Metformin extended release tablets |
WO2007149797A2 (en) | 2006-06-19 | 2007-12-27 | Novartis Ag | Use of organic compounds |
WO2007148185A2 (en) | 2006-06-21 | 2007-12-27 | Pfizer Products Inc. | Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors |
AT503443B1 (en) | 2006-06-23 | 2007-10-15 | Leopold Franzens Uni Innsbruck | Preparation of an ice surface, useful for ice rink, and ice sports cars and trains, comprises freezing water in which an inorganic substance e.g. ammonia, alkali hydroxide, hydrogen halide, nitric acid and sulfuric acid, is added |
TW200811140A (en) | 2006-07-06 | 2008-03-01 | Arena Pharm Inc | Modulators of metabolism and the treatment of disorders related thereto |
TW200811147A (en) | 2006-07-06 | 2008-03-01 | Arena Pharm Inc | Modulators of metabolism and the treatment of disorders related thereto |
US8071583B2 (en) | 2006-08-08 | 2011-12-06 | Boehringer Ingelheim International Gmbh | Pyrrolo[3,2-D] pyrimidines as DPP-IV inhibitors for the treatment of diabetes mellitus |
US8039441B2 (en) | 2006-08-15 | 2011-10-18 | Boehringer Ingelheim International Gmbh | Glucopyranosyl-substituted cyclopropylbenzene derivatives, pharmaceutical compositions containing such compounds, their use as SGLT inhibitors and process for their manufacture |
JP2010501010A (en) | 2006-08-17 | 2010-01-14 | ウェルスタット セラピューティクス コーポレイション | Combination treatment for metabolic disorders |
DE102006042586B4 (en) | 2006-09-11 | 2014-01-16 | Betanie B.V. International Trading | Process for the microparticulate loading of high polymer carbohydrates with hydrophobic active fluids |
WO2008055870A1 (en) | 2006-11-06 | 2008-05-15 | Boehringer Ingelheim International Gmbh | Glucopyranosyl-substituted benzyl-benzonitrile derivatives, medicaments containing such compounds, their use and process for their manufacture |
US7956201B2 (en) | 2006-11-06 | 2011-06-07 | Hoffman-La Roche Inc. | Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one |
NZ598778A (en) | 2006-11-09 | 2013-09-27 | Boehringer Ingelheim Int | Combination therapy with SGLT-2 inhibitors and their pharmaceutical compositions |
CN101657471B (en) | 2006-12-06 | 2013-07-03 | 史密丝克莱恩比彻姆公司 | Bicyclic compounds and use as antidiabetics |
ES2319596B1 (en) | 2006-12-22 | 2010-02-08 | Laboratorios Almirall S.A. | NEW DERIVATIVES OF THE AMINO-NICOTINIC AND AMINO-ISONICOTINIC ACIDS. |
US7638541B2 (en) | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
PE20081849A1 (en) | 2007-01-04 | 2009-01-26 | Prosidion Ltd | PIPERIDIN-4-IL-PROPOXY-BENZAMIDE DERIVATIVES AS GPCR AGONISTS |
CL2008000133A1 (en) | 2007-01-19 | 2008-05-23 | Boehringer Ingelheim Int | PHARMACEUTICAL COMPOSITION THAT INCLUDES A COMPOUND DERIVED FROM PIRAZOL-O-GLUCOSIDE COMBINED WITH AT LEAST A SECOND THERAPEUTIC AGENT; AND USE OF THE COMPOSITION FOR THE TREATMENT OF MELLITUS DIABETES, CATARATS, NEUROPATHY, MYOCARDIAL INFARTS, AND |
UA95828C2 (en) | 2007-02-01 | 2011-09-12 | Такеда Фармасьютикал Компани Лимитед | Solid preparation comprising alogliptin and pioglitazone |
TW200836774A (en) | 2007-02-01 | 2008-09-16 | Takeda Pharmaceutical | Solid preparation |
DE602008006679D1 (en) | 2007-02-06 | 2011-06-16 | Chelsea Therapeutics Inc | NEW COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND THEIR USE |
JP2010521492A (en) | 2007-03-15 | 2010-06-24 | ネクティド,インク. | Anti-diabetic combination comprising sustained release biguanide composition and immediate dipeptidyl peptidase IV inhibitor composition |
CN103330939A (en) | 2007-04-03 | 2013-10-02 | 田边三菱制药株式会社 | Combined use of dipeptidyl peptidase iv inhibitor compound and sweetener |
US9050123B2 (en) | 2007-04-16 | 2015-06-09 | Smith & Nephew, Inc. | Powered surgical system |
PE20090696A1 (en) | 2007-04-20 | 2009-06-20 | Bristol Myers Squibb Co | CRYSTALLINE FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING THEM |
ES2388967T3 (en) | 2007-05-04 | 2012-10-22 | Bristol-Myers Squibb Company | Agonists [6,6] - and [6,7] -cyclics of the GPR119 receptor coupled to the G protein |
WO2007135196A2 (en) | 2007-07-09 | 2007-11-29 | Symrise Gmbh & Co. Kg | Stable soluble salts of phenylbenzimidazole sulfonic acid at phs at or below 7.0 |
ES2603879T3 (en) | 2007-07-19 | 2017-03-01 | Takeda Pharmaceutical Company Limited | Solid preparation comprising alogliptin and metformin hydrochloride |
PE20090597A1 (en) | 2007-08-16 | 2009-06-06 | Boehringer Ingelheim Int | PHARMACEUTICAL COMPOSITION INCLUDING A DERIVATIVE OF PIRAZOL-O-GLUCOSIDE |
CL2008002425A1 (en) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Pharmaceutical composition comprising an inhibitor of sglt2 and 1- (4-methyl-quinazolin-2-yl) methyl-3-methyl-7 - (- 2-butin-1-yl) -8- (3- (r) -amino- Piperidin-1yl) -xanthine, an iv dpp inhibitor and its use for the treatment of obesity and type 1 and 2 diabetes and complications thereof. |
PE20090938A1 (en) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | PHARMACEUTICAL COMPOSITION INCLUDING A BENZENE DERIVATIVE SUBSTITUTED WITH GLUCOPYRANOSIL |
CL2008002424A1 (en) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Pharmaceutical composition comprising a compound derived from pyrazole-o-glucoside; and use of the pharmaceutical composition for the treatment of diabetes mellitus, abnormal glucose tolerance and hyperglycemia, metabolic disorders, among others. |
EP3542801A1 (en) | 2007-08-17 | 2019-09-25 | Boehringer Ingelheim International GmbH | Purin derivatives for use in the treatment of fap-related diseases |
US8338450B2 (en) | 2007-09-21 | 2012-12-25 | Lupin Limited | Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors |
JP5241849B2 (en) | 2007-11-16 | 2013-07-17 | ノボ・ノルデイスク・エー/エス | Pharmaceutical composition comprising insulin and insulinotropic peptide |
CN101234105A (en) | 2008-01-09 | 2008-08-06 | 北京润德康医药技术有限公司 | Pharmaceutical composition containing diabetosan and vildagliptin and preparation thereof |
US20090186086A1 (en) | 2008-01-17 | 2009-07-23 | Par Pharmaceutical, Inc. | Solid multilayer oral dosage forms |
CL2008003653A1 (en) | 2008-01-17 | 2010-03-05 | Mitsubishi Tanabe Pharma Corp | Use of a glucopyranosyl-derived sglt inhibitor and a selected dppiv inhibitor to treat diabetes; and pharmaceutical composition. |
TW200936136A (en) | 2008-01-28 | 2009-09-01 | Sanofi Aventis | Tetrahydroquinoxaline urea derivatives, their preparation and their therapeutic application |
JP2011510986A (en) | 2008-02-05 | 2011-04-07 | メルク・シャープ・エンド・ドーム・コーポレイション | Combination pharmaceutical composition of metformin and dipeptidyl peptidase-IV inhibitor |
EP2259676A4 (en) | 2008-03-04 | 2011-03-16 | Merck Sharp & Dohme | Pharmaceutical compositions of a combination of metformin and a dipeptidyl peptidase-iv inhibitor |
AU2009220615B2 (en) | 2008-03-05 | 2013-12-19 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
US8551524B2 (en) | 2008-03-14 | 2013-10-08 | Iycus, Llc | Anti-diabetic combinations |
ES2543358T3 (en) | 2008-03-31 | 2015-08-18 | Cymabay Therapeutics, Inc. | Oxymethylene aryl compounds and uses thereof |
PE20091730A1 (en) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | FORMULATIONS INVOLVING A DPP4 INHIBITOR |
CN101590007A (en) | 2008-05-27 | 2009-12-02 | 北京瑞伊人科技发展有限公司 | A kind of metformin hydrochloride/voigelibo sugar-lowering oral preparation compositions and preparation thereof |
PE20100156A1 (en) | 2008-06-03 | 2010-02-23 | Boehringer Ingelheim Int | NAFLD TREATMENT |
KR20200118243A (en) | 2008-08-06 | 2020-10-14 | 베링거 인겔하임 인터내셔날 게엠베하 | Treatment for diabetes in patients inappropriate for metformin therapy |
UY32030A (en) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "TREATMENT FOR DIABETES IN INAPPROPRIATE PATIENTS FOR THERAPY WITH METFORMIN" |
PE20110297A1 (en) | 2008-08-15 | 2011-05-26 | Boehringer Ingelheim Int | DPP-4 INHIBITORS FOR WOUND HEALING |
JP2010053576A (en) | 2008-08-27 | 2010-03-11 | Sumitomo Forestry Co Ltd | Mat for paving |
KR20110067096A (en) | 2008-09-10 | 2011-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | Combination therapy for the treatment of diabetes and related conditions |
UY32177A (en) | 2008-10-16 | 2010-05-31 | Boehringer Ingelheim Int | TREATMENT OF DIABETES IN PATIENTS WITH INSUFFICIENT GLUCEMIC CONTROL TO WEIGHT THERAPY WITH DRUG, ORAL OR NOT, ANTIDIABÉTICO |
WO2010045656A2 (en) | 2008-10-17 | 2010-04-22 | Nectid, Inc. | Novel sglt2 inhibitor dosage forms |
JP2012512848A (en) | 2008-12-23 | 2012-06-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Salt forms of organic compounds |
AR074990A1 (en) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | TREATMENT OF DIABETES IN PATIENTS WITH AN INAPPROPRIATE GLUCEMIC CONTROL THROUGH METFORMIN THERAPY |
TWI466672B (en) | 2009-01-29 | 2015-01-01 | Boehringer Ingelheim Int | Treatment for diabetes in paediatric patients |
NZ594044A (en) | 2009-02-13 | 2014-08-29 | Boehringer Ingelheim Int | Antidiabetic medications comprising a dpp-4 inhibitor (linagliptin) optionally in combination with other antidiabetics |
UY32427A (en) | 2009-02-13 | 2010-09-30 | Boheringer Ingelheim Internat Gmbh | PHARMACEUTICAL COMPOSITION, PHARMACEUTICAL FORM, PROCEDURE FOR PREPARATION, METHODS OF TREATMENT AND USES OF THE SAME |
WO2010092125A1 (en) | 2009-02-13 | 2010-08-19 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof |
TW201031661A (en) | 2009-02-17 | 2010-09-01 | Targacept Inc | Fused benzazepines as neuronal nicotinic acetylcholine receptor ligands |
EP2408780A2 (en) | 2009-03-20 | 2012-01-25 | Pfizer Inc. | 3-oxa-7-azabicycloý3.3.1¨nonanes |
US8815292B2 (en) | 2009-04-27 | 2014-08-26 | Revalesio Corporation | Compositions and methods for treating insulin resistance and diabetes mellitus |
BRPI1013992A2 (en) | 2009-04-27 | 2016-08-16 | Revalesio Corp | compositions and methods for treating insulin resistance and diabetes mellitus |
US20120100221A1 (en) | 2009-06-02 | 2012-04-26 | Ranbaxy Laboratories Limited | Pharmaceutical compositions containing a combination of an antihistamine and a decongestant |
WO2010147768A1 (en) | 2009-06-15 | 2010-12-23 | Merck Sharp & Dohme Corp. | Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone |
MX2012000892A (en) | 2009-07-21 | 2012-06-01 | Keryx Biopharmaceuticals Inc | Ferric citrate dosage forms. |
CN102596191B (en) | 2009-10-02 | 2016-12-21 | 勃林格殷格翰国际有限公司 | Comprise the pharmaceutical composition of BI 1356 and metformin |
UY32919A (en) | 2009-10-02 | 2011-04-29 | Boehringer Ingelheim Int | Pharmaceutical composition, pharmaceutical dosage form, procedure for its preparation, methods for its treatment and its uses |
JP5446716B2 (en) | 2009-10-21 | 2014-03-19 | 大正製薬株式会社 | Method for producing tablets containing arginine and carnitine |
BR112012012641A2 (en) | 2009-11-27 | 2020-08-11 | Boehringer Ingelheim International Gmbh | TREATMENT OF GENOTYPED DIABETIC PATIENTS WITH DPP-lVTAL INHIBITORS LIKE LINAGLIPTIN |
JP2010070576A (en) | 2009-12-28 | 2010-04-02 | Sato Pharmaceutical Co Ltd | Rapidly soluble tablet |
TWI562775B (en) | 2010-03-02 | 2016-12-21 | Lexicon Pharmaceuticals Inc | Methods of using inhibitors of sodium-glucose cotransporters 1 and 2 |
WO2011113947A1 (en) | 2010-03-18 | 2011-09-22 | Boehringer Ingelheim International Gmbh | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
WO2011138421A1 (en) | 2010-05-05 | 2011-11-10 | Boehringer Ingelheim International Gmbh | Combination therapy |
CN102883711A (en) | 2010-05-05 | 2013-01-16 | 贝林格尔.英格海姆国际有限公司 | Pharmaceutical formulations comprising pioglitazone and linagliptin |
ES2577930T3 (en) | 2010-06-09 | 2016-07-19 | Poxel | Triazine derivatives to delay the onset of type 1 diabetes |
MX2012015188A (en) | 2010-06-22 | 2013-05-20 | Twi Pharmaceuticals Inc | Controlled release compositions with reduced food effect. |
EP3366304B1 (en) | 2010-06-24 | 2020-05-13 | Boehringer Ingelheim International GmbH | Diabetes therapy |
CN103370064A (en) | 2010-09-03 | 2013-10-23 | 百时美施贵宝公司 | Drug formulations using water soluble antioxidants |
WO2012039420A1 (en) | 2010-09-21 | 2012-03-29 | 国立大学法人九州大学 | Bionic aortic baroreflex system for treating disease associated with aortic baroreflex dysfunction |
US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
WO2012088682A1 (en) | 2010-12-29 | 2012-07-05 | Shanghai Fochon Pharmaceutical Co Ltd. | 2-(3-aminopiperidin-1-yl)-[1,2,4]triazolo[1,5-c]pyrimidine-5,7(3h,6h)-dione derivates as dipeptidyl peptidase iv(dpp-iv) inhibitors |
MX2013008372A (en) | 2011-02-01 | 2013-08-12 | Astrazeneca Uk Ltd | Pharmaceutical formulations including an amine compound. |
AR085689A1 (en) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | PHARMACEUTICAL COMPOSITIONS OF METFORMIN, LINAGLIPTINE AND AN SGLT-2 INHIBITOR |
JP6028016B2 (en) | 2011-05-10 | 2016-11-16 | サンド・アクチエンゲゼルシヤフト | Polymorphs of linagliptin benzoate |
WO2013010964A1 (en) | 2011-07-15 | 2013-01-24 | Boehringer Ingelheim International Gmbh | Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions |
US20130172244A1 (en) | 2011-12-29 | 2013-07-04 | Thomas Klein | Subcutaneous therapeutic use of dpp-4 inhibitor |
CN106968050B (en) | 2012-01-04 | 2019-08-27 | 宝洁公司 | Fibre structure containing active material with multiple regions |
US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
US20130303554A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in sirs and/or sepsis |
WO2013171167A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
EP2854812A1 (en) | 2012-05-24 | 2015-04-08 | Boehringer Ingelheim International GmbH | A xanthine derivative as dpp -4 inhibitor for use in the treatment of autoimmune diabetes, particularly lada |
WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
WO2013174769A1 (en) | 2012-05-25 | 2013-11-28 | Boehringer Ingelheim International Gmbh | Use of keratinocytes as a biologically active substance in the treatment of wounds, such as diabetic wounds, optionally in combination with a dpp-4 inhibitor |
WO2013179307A2 (en) | 2012-05-29 | 2013-12-05 | Mylan Laboratories Limited | Stabilized pharmaceutical compositions of saxagliptin |
AU2013304949C1 (en) | 2012-08-24 | 2020-12-24 | Novartis Ag | NEP inhibitors for treating diseases characterized by atrial enlargement or remodeling |
WO2014056942A1 (en) | 2012-10-09 | 2014-04-17 | Boehringer Ingelheim International Gmbh | Use of selectively moisture-adjusted tabletting material in the production of mechanically stable tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing tablets |
JP2015533133A (en) | 2012-10-09 | 2015-11-19 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Use of moisture-control disintegrants in tablet manufacture |
US9050302B2 (en) | 2013-03-01 | 2015-06-09 | Jazz Pharmaceuticals Ireland Limited | Method of administration of gamma hydroxybutyrate with monocarboxylate transporters |
CN110075098A (en) | 2013-03-15 | 2019-08-02 | 勃林格殷格翰国际有限公司 | Purposes of the Li Gelieting in heart and protection renal antidiabetic treatment |
EA033286B1 (en) | 2013-04-18 | 2019-09-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Method of treating or delaying the progression of chronic kidney disease |
US20140343014A1 (en) | 2013-05-17 | 2014-11-20 | Boehringer Ingelheim International Gmbh | Combination of a certain dpp-4 inhibitor and voglibose |
WO2014198906A1 (en) | 2013-06-14 | 2014-12-18 | Boehringer Ingelheim International Gmbh | Dpp-4 inhibitors for treating diabetes and its complications |
ES2950384T3 (en) | 2014-02-28 | 2023-10-09 | Boehringer Ingelheim Int | Medical use of a DPP-4 inhibitor |
CN104130258B (en) | 2014-08-13 | 2016-06-01 | 广东东阳光药业有限公司 | The method for transformation of a kind of dimer |
WO2016059219A1 (en) | 2014-10-17 | 2016-04-21 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
EP3468562A1 (en) | 2016-06-10 | 2019-04-17 | Boehringer Ingelheim International GmbH | Combinations of linagliptin and metformin |
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